Search Result
Results for "
Antagonize
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
19
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-19739
-
JW74
5 Publications Verification
|
Wnt
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Cancer
|
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JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling with an IC50 of 420 nM.
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-
-
- HY-N0201
-
|
|
TNF Receptor
Toll-like Receptor (TLR)
JAK
STAT
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Cancer
|
|
Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
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-
-
- HY-19010A
-
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SKF 94482 hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
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BMY-25368 hydrochloride is a histamine H2 receptor antagonist that acts as a gastric acid secretion inhibitor. BMY-25368 hydrochloride competitively antagonizes gastric secretion stimulated by histamine and also antagonizes gastric secretion stimulated by Pentagastrin (HY-A0261), Bethanechol (HY-B0406), and food .
|
-
-
- HY-13596
-
|
51W89 besylate; Cisatracurium besilate
|
nAChR
Autophagy
|
Neurological Disease
Cancer
|
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Cisatracurium besylate (51W89) is a nondepolarizing neuromuscular blocking agent, antagonizing the action of acetylcholine by inhibiting neuromuscular transmission.
|
-
-
- HY-P2499A
-
|
|
Bcl-2 Family
|
Cancer
|
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BAD (103-127) (human), FAM-labeled TFA is a FAM-labeled human BAD (103-127) (HY-P2468). BAD (103-127) (human) TFA, the 25-mer Bad peptide, is derived from the BH3 domain of BAD and can antagonize the function of Bcl-xL .
|
-
-
- HY-W197533
-
|
|
Others
|
Neurological Disease
|
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3-Hydroxymethyl-β-carboline antagonizes the anxiolytic and anticonvulsant actions of Diazepam and reverses the sedative action of Flurazepam. 3-Hydroxymethyl-β-carboline also antagonizes the cerebrovascular and cerebral metabolic depression produced by Flurazepam .
|
-
-
- HY-P5061
-
-
-
- HY-19010
-
|
SKF 94482
|
Histamine Receptor
|
Neurological Disease
|
|
BMY-25368 (SKF 94482) is a histamine H2 receptor antagonist that acts as a gastric acid secretion inhibitor. BMY-25368 competitively antagonizes gastric secretion stimulated by histamine and also antagonizes gastric secretion stimulated by Pentagastrin (HY-A0261), Bethanechol (HY-B0406), and food .
|
-
-
- HY-162285
-
|
|
Akt
|
Cancer
|
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Anticancer agent 189 (compound 4) is an anticancer agent that antagonizes CRC effects by targeting AKT1 .
|
-
-
- HY-P0300
-
|
|
Bcl-2 Family
|
Cancer
|
|
Bak BH3 is derived from the BH3 domain of Bak, can antagonize the function of Bcl-xL in cells.
|
-
-
- HY-131471
-
-
-
- HY-B0098
-
-
-
- HY-B0098A
-
-
-
- HY-137407
-
|
|
Bacterial
|
Infection
|
|
N-Phenylacetyl-L-homoserine lactone is a small diffusible signaling molecule that strongly antagonizes or super-activates the quorum sensing of Vibrio fischeri .
|
-
-
- HY-124232
-
-
-
- HY-U00402
-
-
-
- HY-105960
-
-
-
- HY-123202
-
|
|
P2Y Receptor
|
Cancer
|
|
MRS2603 is a pyridoxal derivative. MRS2603 antagonized both P2Y1 and P2Y13 receptors .
|
-
-
- HY-105960A
-
-
-
- HY-N0201R
-
|
|
TNF Receptor
Reference Standards
Toll-like Receptor (TLR)
JAK
STAT
|
Cancer
|
|
Atractylenolide I (Standard) is the analytical standard of Atractylenolide I. This product is intended for research and analytical applications. Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
|
-
-
- HY-103500
-
-
-
- HY-124779
-
|
(S)-GEA 654; (S)-A03
|
iGluR
|
Neurological Disease
Metabolic Disease
|
|
(S)-Alaproclate ((S)-GEA 654) is more potent than the R-(+)-enantiomer both in blocking the NMDA receptor currents in vitro and in antagonizing the cGMP increase in vivo .
|
-
-
- HY-18732B
-
-
-
- HY-123015
-
|
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Calcium Channel
|
Neurological Disease
|
|
Tamolarizine is a calcium channel blocker. Tamolarizine crosses the blood-brain barrier and antagonizes the effects of calcium on neurons. Tamolarizine can be used in nervous system research .
|
-
-
- HY-18732C
-
|
Tilarginine hydrochloride; Methylarginine hydrochloride
|
NO Synthase
Endogenous Metabolite
|
Cardiovascular Disease
Cancer
|
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L-NMMA (Tilarginine) hydrochloride competitively antagonizes L-arginine, and thus inhibits production of nitric oxide (NO). L-NMMA hydrochloride is utilized as NO synthase antagonist in experimental settings .
|
-
-
- HY-106779
-
|
|
Calcium Channel
|
Neurological Disease
|
|
Tamolarizine hydrochloride is a calcium channel blocker. Tamolarizine hydrochloride crosses the blood-brain barrier and antagonizes the effects of calcium on neurons. Tamolarizine hydrochloride can be used in nervous system research .
|
-
-
- HY-148909
-
|
IDEFP
|
Cannabinoid Receptor
FAAH
|
Neurological Disease
|
|
Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is an organophosphorus ester that antagonizes the central cannabinoid receptor (CB1) and inhibits FAAH with similar potencies (IC50 = 2 nM) .
|
-
-
- HY-124539
-
|
|
iGluR
|
Neurological Disease
|
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ZK 187638 is an AMPA receptor antagonist. ZK 187638 antagonizes the kainate-induced currents in cultured hippocampal neurons with an IC50 of 3.4 μM in a noncompetitive fashion .
|
-
-
- HY-B0098S
-
-
-
- HY-18732
-
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Tilarginine; Methylarginine
|
NO Synthase
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Others
|
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L-NMMA (Tilarginine; Methylarginine) competitively antagonizes L-arginine, and thus inhibits production of nitric oxide (NO). L-NMMA is utilized as NO synthase antagonist in experimental settings .
|
-
-
- HY-164795
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
SBI-810 is a functionally selected β-arrestin-biased neurotensin receptor 1 (NTSR1) allosteric modulator. SBI-810 modulates NTSR1 G protein signaling in a G protein-specific manner in the presence of the endogenous ligand, neurotensin (NT). SBI-810 fully antagonizes NT-induced activation of Gq, partially antagonizes NT-induced activation of Gi1 and is permissive of NTSR1 activation of GoA and G12 .
|
-
-
- HY-115375
-
|
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5-HT Receptor
|
Neurological Disease
|
|
50595 hydrochloride is a selective noncompetitive cisapride antagonist that interferes with the activity of cisapride and BRL 24924. R 50595 hydrochloride has no effect on the response to electrical stimulation at concentrations up to 3 X 10(-7) M. R 50595 hydrochloride antagonizes the effects of cisapride and BRL 24924 in a noncompetitive manner. R 50595 hydrochloride completely abolishes the effects of 5-HT at a concentration of 3 X 10(-7) M and also antagonizes the effects of 5-HT in a noncompetitive manner .
|
-
-
- HY-164795A
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
SBI-810 hydrochloride is a functionally selected β-arrestin-biased neurotensin receptor 1 (NTSR1) allosteric modulator. SBI-810 hydrochloride modulates NTSR1 G protein signaling in a G protein-specific manner in the presence of the endogenous ligand, neurotensin (NT). SBI-810 hydrochloride fully antagonizes NT-induced activation of Gq, partially antagonizes NT-induced activation of Gi1 and is permissive of NTSR1 activation of GoA and G12 .
|
-
-
- HY-119595
-
|
R3201
|
Others
|
Neurological Disease
|
|
Haloperidide (R3201) is a neuroleptic compound. Haloperidide is a potent and selective anti-emetic agent. Haloperidide antagonizes Apomorphine (HY-12723)-induced emesis in dogs .
|
-
-
- HY-P2052
-
|
|
Opioid Receptor
Neurokinin Receptor
|
Others
|
|
AWL 60 is a compound with SP antagonist and weak opioid agonist properties, which can antagonize SP-agonists in vitro and attenuate the decrease in blood pressure caused by SP-agonists in vivo.
|
-
-
- HY-101347
-
|
|
nAChR
|
Neurological Disease
|
|
Chlorisondamine (diiodide) is a potent nicotinic acetylcholine receptor (nAChR) antagonist and a ganglion blocker. Chlorisondamine antagonizes some of nicotine's central actions in a potent, long-lasting and pharmacologically selective way .
|
-
-
- HY-12287
-
-
-
- HY-N0541
-
|
Ginsenoside A1
|
Endogenous Metabolite
|
Others
|
|
Pseudoginsenoside F11 (Ginsenoside A1), a component of Panax quinquefolium (American ginseng), has been demonstrated to antagonize the learning and memory deficits induced by scopolamine, morphine and methamphetamine in mice.
|
-
-
- HY-P2579
-
-
-
- HY-N2197
-
|
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nAChR
|
Neurological Disease
|
|
Hirsuteine is an indole alkaloid extracted from Uncaria rhynchophylla. Hirsuteine non-competitively antagonizes nicotine-mediated dopamine release by blocking ion permeation through nicotinic receptor channel complexes .
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-
-
- HY-P1721
-
|
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Bradykinin Receptor
|
Cardiovascular Disease
|
|
NPC 17731 is a new bradykinin (BK) receptor antagonist. NPC 17731 antagonized both the contractile and relaxant responses caused by BK in longitudinal smooth muscle with IC50 of 23 and 29 nM, respectively .
|
-
-
- HY-15393
-
|
|
mGluR
|
Neurological Disease
|
|
VU 0357121 is a positive and highly selective mGlu5R allosteric modulator (PAM) with an EC50 of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes .
|
-
-
- HY-111006
-
|
UH 232
|
Dopamine Receptor
|
Neurological Disease
|
|
(+)-UH 232 is a partially selective agonist of the D3 receptor with an intrinsic activity of 0.2-0.4. (+)-UH 232 antagonized quinpirole-induced mitogenesis with a Ki value of 9.4 nM .
|
-
-
- HY-N13994
-
|
|
Fungal
|
Infection
|
|
Clavamycin A has strong anti-candida activity, and its action can be antagonized by dipeptide or tripeptide, but amino acid can not cancel its action. No antibacterial activity and no inhibition of β-lactamase .
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-
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- HY-N3320
-
|
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Others
|
Neurological Disease
|
|
Marmin is a coumarin, that can be isolated from the immature bark of Aegle marmelos Correa. Marmin antagonizes the Histamine (HY-B1204)-induced contraction in competitive manner .
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-
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- HY-N13997
-
|
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Fungal
|
Infection
|
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Clavamycin C has strong anti-candida activity, and its action can be antagonized by dipeptide or tripeptide, but amino acid can not cancel its action. No antibacterial activity and no inhibition of β-lactamase .
|
-
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- HY-19007
-
|
DA 4577
|
Histamine Receptor
|
Endocrinology
|
|
Mifentidine (DA 4577) is a potent and selective H2 Receptor antagonist. Mifentidine has an anti-secretion effect and can antagonize the acid-promoting activity of histamine with EC50 3.28 μM .
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-
-
- HY-N13999
-
|
|
Fungal
|
Infection
|
|
Clavamycin D has strong anti-candida activity, and its action can be antagonized by dipeptide or tripeptide, but amino acid can not cancel its action. No antibacterial activity and no inhibition of β-lactamase .
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-
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- HY-129474
-
|
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Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
MP 518 is a PDE inhibitor with antihypertensive properties. MP 518 can inhibit cAMP degradation, causing an increase in ICa, and can also antagonize β-adrenergic stimulation, exerting vasodilation .
|
-
-
- HY-120979
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
NO-Losartan A (compound 2a) displays vasorelaxing effects, due to the release of NO, and antagonized the vasocontractile effects of Angiotensin II (HY-13948), with potency values similar to that of Losartan (HY-17512) .
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-
- HY-B0745
-
-
- HY-N13996
-
|
|
Fungal
|
Infection
|
|
Clavamycin B has strong anti-candida activity, and its action can be antagonized by dipeptide or tripeptide, but amino acid can not cancel its action. No antibacterial activity and no inhibition of β-lactamase .
|
-
- HY-B0098AR
-
-
- HY-135108
-
|
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Neurokinin Receptor
|
Neurological Disease
|
|
QWF Peptide (Compound 4a) is a substance P antagonist with an IC50 of 0.09 μM. QWF Peptide antagonizes the SP-induced contraction of isolated guinea pig trachea strips with an IC50 of 4.7 μM .
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-
- HY-P1471
-
|
22-52-Adrenomedullin (human)
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (AM) (22-52), human, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist, and also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat .
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- HY-118416
-
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Opioid Receptor
|
Neurological Disease
|
|
BMS-986124 is a μ-opioid receptor silent allosteric modulator (μ-SAMs). BMS-986124 antagonizes positive allosteric modulator effect of BMS-986122 (µ-OR PAM) .
|
-
- HY-105236
-
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(Rac)-CI-977 free base
|
Opioid Receptor
|
Neurological Disease
|
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(Rac)-Enadoline ((Rac)-CI-977 free base) is a selective K-opioid receptor agonist that stereoselectively antagonizes clonic seizures induced by slow intravenous injection of N-methyl-DL-aspartate in mice .
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-
- HY-13596R
-
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51W89 besylate (Standard); Cisatracurium besilate (Standard)
|
Reference Standards
nAChR
Autophagy
|
Neurological Disease
Cancer
|
|
Cisatracurium (besylate) (Standard) is the analytical standard of Cisatracurium (besylate). This product is intended for research and analytical applications. Cisatracurium besylate (51W89) is a nondepolarizing neuromuscular blocking agent, antagonizing the action of acetylcholine by inhibiting neuromuscular transmission.
|
-
- HY-P3853
-
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Neurokinin Receptor
|
Neurological Disease
|
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GR 87389 is a potent NK2 receptor antagonist. GR 87389 antagonized GA 64349-induced smooth muscle strips contractions in a competitive manner in the human detrusor, prostate and prostatic urethra .
|
-
- HY-15064
-
HC-030031
Maximum Cited Publications
33 Publications Verification
|
TRP Channel
|
Neurological Disease
|
|
HC-030031 is a potent and selective TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.
|
-
- HY-A0215
-
|
BW-A 938U; Nuromax
|
nAChR
|
Neurological Disease
|
|
Doxacurium chloride (BW A938U) is a potent non-depolarizing neuromuscular blocking agent. Doxacurium chloride binds to cholinergic receptors to antagonize acetylcholine, resulting in a block of neuromuscular transmission. Doxacurium chloride can be used for the research of neurological diseases .
|
-
- HY-148758
-
-
- HY-50001
-
|
|
Influenza Virus
|
Infection
|
|
Nucleozin, a potent inhibitor of influenza A virus infection, induces the formation of nucleoprotein (NP) aggregates and antagonizes its nuclear accumulation, leading to cessation of viral replication. Nucleozin impedes influenza A virus replication in vitro with a nanomolar EC50 .
|
-
- HY-P2436
-
|
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Neurokinin Receptor
|
Neurological Disease
|
|
L-659837 is a NK2 receptor antagonist, and can antagonize GR 64349 (HY-P1278)-induced contraction. L-659837 can be used for study of urinary bladder disorders .
|
-
- HY-13848
-
-
- HY-P99514
-
|
AGEN1884
|
CTLA-4
|
Cancer
|
|
Zalifrelimab (AGEN1884) is a fully human IgG1 monoclonal antibody targeting CTLA-4 (CTLA-4). Zalifrelimab antagonizes the inhibitory checkpoints of immune cell activation regulated by CTLA-4 signaling .
|
-
- HY-15001A
-
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SR1 hydrochloride
|
Aryl Hydrocarbon Receptor
|
Others
|
|
Stemregenin 1 hydrochloride is a purine derivative that antagonizes aryl hydrocarbon receptor signaling in CD34+ cells. IC50 The value is 127 nM. Stemregenin 1 hydrochloride can be used to expand the pluripotency of hematopoietic stem cells (HSC) in stem cell studies .
|
-
- HY-101622
-
-
- HY-15872A
-
|
|
Farnesyl Transferase
Apoptosis
Ras
|
Infection
Cancer
|
|
FTI-277 hydrochloride is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling. FTI-277 hydrochloride can inhibit hepatitis delta virus (HDV) infection.
|
-
- HY-106347
-
|
CR 2945
|
Cholecystokinin Receptor
|
Inflammation/Immunology
|
|
Itriglumide (CR 2945) is an anthranilic acid derivative. Itriglumide is a potent and selective CCKB receptor antagonist, with an IC50 of 2.3 nM. Itriglumide antagonizes the response to gastrin in a dose-dependent manner with an IC50 of 5.9 nM. Itriglumide shows antisecretory and antiulcer activity .
|
-
- HY-101946
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively, and has antiallergic activities.
|
-
- HY-15872
-
|
|
Farnesyl Transferase
Apoptosis
Ras
|
Infection
Cancer
|
|
FTI-277 is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling. FTI-277 can inhibit hepatitis delta virus (HDV) infection.
|
-
- HY-D2259
-
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|
E1/E2/E3 Enzyme
|
Others
|
|
PFI-7 is a probe, which binds to human GID4 (KD is 79 nM), and antagonizes the binding of Pro/N-degrons. PFI-7 can be utilized in C-terminal to LisH (CTLH) complex research and development of targeted protein degradation .
|
-
- HY-19642
-
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MGCD265
|
TAM Receptor
c-Met/HGFR
|
Cancer
|
|
Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) .
|
-
- HY-19642A
-
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MGCD265 hydrochloride
|
TAM Receptor
c-Met/HGFR
|
Cancer
|
|
Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) .
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-
- HY-160765
-
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APS-8-100-2
|
Wnt
Apoptosis
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Cancer
|
|
WNTinib (APS-8-100-2) is a multi-kinase inhibitor that selectively antagonizes β-catenin (CTNNB1) mutated hepatocellular carcinoma (HCC). WNTinib downregulates oncogenicWntsignaling by inhibiting KIT/MAPK and downstream EZH2 activation .
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-
- HY-115594
-
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STAT
Apoptosis
|
Cancer
|
|
Erasin is a potent Erlotinib (HY-50896)-resistance antagonizing STAT3 inhibitor with IC50s of 9.7 and 24 μM against STAT3 and STAT1, respectively. Erasin induces cancer cells apoptosis .
|
-
- HY-B1573A
-
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AY-23,028; dl-Butaclamol hydrochloride
|
Adrenergic Receptor
Dopamine Receptor
|
Neurological Disease
|
|
(±)-Butaclamol hydrochloride (AY-23,028) is the antagonist for adrenergic receptor and dopamine receptor. (±)-Butaclamol hydrochloride antagonizes amphetamine or Apomorphine (HY-12723)-induced stereotyped behaviors and emesis, inhibits discriminative avoidance behavior, and induces catalepsy in rats models .
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-
- HY-117937
-
BC-1215
2 Publications Verification
|
Ligands for E3 Ligase
|
Inflammation/Immunology
|
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BC-1215 is a F-box protein 3 (Fbxo3) inhibitor. BC-1215 works by antagonizing of Fbxo3 on TRAF cytokine signaling and exhibits a low IC50 in vitro. BC-1215 can be used for the research of inflammation .
|
-
- HY-P10619
-
-
![[Tyr6,D-Phe7,D-His9]-Substance P (6-11)](//file.medchemexpress.eu/product_pic/hy-p10619.gif)
- HY-B0745S
-
-
- HY-110038
-
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Farnesyl Transferase
Apoptosis
Ras
|
Infection
Cancer
|
|
FTI-277 TFA is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling. FTI-277 TFA can inhibit hepatitis delta virus (HDV) infection.
|
-
- HY-P1329
-
|
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Opioid Receptor
|
Neurological Disease
|
|
CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .
|
-
- HY-157891
-
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Apoptosis
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Cancer
|
|
JBC117 is a novel anticancer lead compound targeting Pygo2 PHD. JBC117 can effectively antagonize the cell effect of β-catenin-dependent activity and inhibit the migration and invasion of cancer cells. JBC117 can induce apoptosis .
|
-
- HY-148695B
-
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Interleukin Related
|
Inflammation/Immunology
|
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ADR58 sodium is a highly potent and selective human oncostatin M (OSM) antagonist, which can prevent the binding of OSM to the gp130 receptor and specifically antagonize OSM-mediated signaling. ADR58 sodium can be used in the research of rheumatoid arthritis related diseases .
|
-
- HY-P2429
-
|
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Opioid Receptor
|
Others
|
|
N,N-Diallyl-Tyr-Aib-Aib-Phe-Leu is a compound that can antagonize the δ-opioid receptor and the action of [D-Pen2,D-Pen ] enkephalin in vivo. Its antagonistic effect can be verified by specific behavioral experiments.
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-
- HY-148695C
-
|
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Interleukin Related
|
Inflammation/Immunology
|
|
ADR58 sodium is a highly potent and selective human oncostatin M (OSM) antagonist, which can prevent the binding of OSM to the gp130 receptor and specifically antagonize OSM-mediated signaling. ADR58 sodium can be used in the research of rheumatoid arthritis related diseases .
|
-
- HY-107653
-
|
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mAChR
|
Neurological Disease
|
|
J 104129 fumarate is a selective and orally active muscarinic M3 antagonist with Ki values of 4.2 nM and 490 nM for M3 and M2, respectively. J 104129 fumarate antagonized ACh-induced bronchoconstriction. J 104129 fumarate has the potential for the research of obstructive airway disease .
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-
- HY-114542
-
|
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Drug Derivative
|
Others
|
|
LY 201409 is an anticonvulsant compound that is an analog of LY-201116 (HY-114705) with improved metabolic activity. LY 201409 antagonizes maximal electroconvulsive-induced seizures, has mixed effects on seizures induced by multiple chemoconvulsants, and affects behavior and sleep in mice .
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-
- HY-116814
-
|
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EBI2/GPR183
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Inflammation/Immunology
|
|
ML401, a potent chemical probe, selectively antagonizes EBI2 (also known as GPR183) with an IC50 of 1.03 nM. ML401 displays activity in a chemotaxis assay (IC50=6.24 nM). ML401 shows good stability and no toxicity .
|
-
- HY-141644
-
|
|
Annexin A
YAP
|
Inflammation/Immunology
|
|
PY-60 is a robust and specific activator of YAP transcriptional activity that targets annexin A2 (ANXA2) with a Kd of 1.4 µM. PY-60 directly binds to ANXA2 and antagonizes its normal cellular function of repressing YAP activity .
|
-
- HY-108295
-
|
CXB-722
|
GABA Receptor
|
Neurological Disease
|
|
Pivagabine (CXB 722) is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. Pivagabine penetrates the blood-brain barrier in rats. Pivagabine antagonizes the effects of foot shock on both GABAA receptor function and corticotropin-releasing factor (CRF) concentrations in rat brain .
|
-
- HY-172149
-
|
5'-NTII
|
Opioid Receptor
|
Neurological Disease
|
|
Naltrindole 5′-isothiocyanate (5'-NTII) is a non-selective delta opioid receptor antagonist that can antagonize the analgesic effects induced by DSLET (HY-P1332) without affecting the analgesic effects induced by DPDPE (HY-P1334) .
|
-
- HY-170447
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NOD1 antagonist-2 (compound 66) is an orally active selective antagonist of both human and mouse NOD1. NOD1 antagonist-2 (compound 66) antagonizes NOD1-induced NF-κB and MAPK pathways .
|
-
- HY-P1329A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity .
|
-
- HY-123103
-
|
|
Lipoxygenase
Histamine Receptor
|
Inflammation/Immunology
|
|
Linetastine is an orally active and potent 5-Lipoxygenase inhibitor. Linetastine shows antihistamine activity. Linetastine inhibits leukotriene production and antagonizes the effect of histamine. Linetastine inhibits the release of leukotrienes B4 and C4 from calcium ionophore-stimulated human leukocytes .
|
-
- HY-148349
-
-
- HY-B1382
-
|
1,2,2,6,6-Pentamethylpiperidine
|
nAChR
|
Cardiovascular Disease
Neurological Disease
|
|
Pempidine (1,2,2,6,6-Pentamethylpiperidine) is an orally active ganglionic blocking agent used in hypertension-related conditions. Pempidine is a nicotinic receptor blocker. Pempidine can antagonize the nicotine-induced increase of the striatal dopamine (DA) in vitro .
|
-
- HY-137111
-
|
|
5-HT Receptor
PERK
|
|
|
p-MPPF dihydrochloride is a selective 5-HT antagonist that dose-dependently antagonizes the reduction of phosphorylated Erk1/2 levels in the hippocampus induced by 8-OH-DPAT (HY-112061) in rats. p-MPPF dihydrochloride can be used for neurological disease research .
|
-
- HY-137111A
-
|
|
5-HT Receptor
PERK
|
|
|
p-MPPF is a selective 5-HT antagonist that dose-dependently antagonizes the reduction of phosphorylated Erk1/2 levels in the hippocampus induced by 8-OH-DPAT (HY-112061) in rats. p-MPPF can be used for neurological disease research .
|
-
- HY-18660
-
|
PER977
|
Factor Xa
Thrombin
|
Cardiovascular Disease
|
|
Ciraparantag (PER977) is a thrombin and factor Xa inhibitor. Ciraparantag is a broad-spectrum reversal agent for anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants. It is reported to antagonize the effects of all coagulants except VKAs and agratroban .
|
-
- HY-P10631
-
|
|
HSP
|
Inflammation/Immunology
|
|
Gp96-II is a gp96-blocking peptide that antagonizes gp96-mediated LPS(HY-D1056)-induced cytokine production. Gp96-II can be utilized in research on inflammatory disease .
|
-
- HY-P99659
-
|
ANB 019
|
Interleukin Related
|
Inflammation/Immunology
|
|
Imsidolimab (ANB 019) is a high-affinity, humanized monoclonal antibody of anti-IL-36R. Imsidolimab antagonizes IL-36 cytokine signal transduction. Imsidolimab has potential application in generalized pustular psoriasis (GPP) and other inflammatory skin diseases .
|
-
- HY-B0267C
-
|
Aroxybutynin
|
mAChR
|
Neurological Disease
|
|
(R)-Oxybutynin (Aroxybutynin) is the racemic isomer of Oxybutynin and an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antispasmodic, antimuscarinic, and anticholinergic activities and competitively antagonizes carbachol-induced contractions. (R)-Oxybutynin can be used to study urinary incontinence caused by neurogenic bladder dysfunction .
|
-
- HY-P1471A
-
|
22-52-Adrenomedullin (human) (TFA)
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. Adrenomedullin (AM) (22-52), human also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat .
|
-
- HY-120954
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
14,15-EE-5(Z)-E is a structural analogue of 14, 15-epoxide dicartrienoic acid (14,15-EET). 14,15-EE-5(Z)-E antagonizes the relaxation of vascular smooth muscle induced by EET .
|
-
- HY-P2499
-
|
|
Bcl-2 Family
|
Cancer
|
|
BAD (103-127) (human), FAM-labeled is a FAM-labeled human BAD (103-127) (HY-P2468). BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD and can antagonize the function of Bcl-xL .
|
-
- HY-15065
-
-
- HY-18959
-
|
|
β-catenin
Wnt
|
Cancer
|
|
CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs) .
|
-
- HY-125408
-
|
MCTR1
|
Leukotriene Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Maresin conjugates in tissue regeneration 1 (MCTR1) is a potent cytokine of pro-resolving mediating maresin conjugates in tissue regeneration (MCTR), which reduces the inflammatory response and promotes tissue regeneration. Maresin conjugates in tissue regeneration 1 antagonize LTD4-stimulated vascular responses .
|
-
- HY-W010062
-
|
|
Drug Derivative
Cytochrome P450
Estrogen Receptor/ERR
|
Metabolic Disease
Cancer
|
|
4-Chlorophenylacetic acid is a halogenated phenylacetic acid derivative. 4-Chlorophenylacetic acid is a potent aromatase inhibitor and antagonizes estrogen signaling. 4-Chlorophenylacetic acid can provide carbon and energy for Pseudomonas sp. strain CBS3. 4-Chlorophenylacetic acid is effective against estrogen-induced mammary tumorigenesis .
|
-
- HY-P1108
-
|
|
CFTR
|
Others
|
|
Astressin 2B is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B antagonizes CRF2-mediated inhibition of gastric emptying .
|
-
- HY-103319
-
|
R 24571
|
Autophagy
Calmodulin
|
Neurological Disease
Cancer
|
|
Calmidazolium chloride (R 24571) is a calmodulin antagonist, antagonizing CaM-dependent phosphodiesterase and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively . Also in anti-cancer research . Calmidazolium binds to calmodulin with a Kd of 3 nM.
|
-
- HY-18660A
-
|
PER977 TFA
|
Factor Xa
Thrombin
|
Cardiovascular Disease
|
|
Ciraparantag (PER977) TFA is a thrombin and factor Xa inhibitor. Ciraparantag TFA is a broad-spectrum reversal agent for anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants. It is reported to antagonize the effects of all coagulants except VKAs and agratroban .
|
-
- HY-16935
-
|
JNJ-39439335
|
TRP Channel
|
Neurological Disease
|
|
Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca 2+ influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain .
|
-
- HY-113758
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
LY 163443 is a selective antagonist of leukotrienes D4 (LTD4) and E4 (LTE4). LY 163443 can antagonize LTD4-induced contractions of guinea pig ileum, trachea, and lung parenchyma. LY 163443 also inhibits tracheal contractions to LTE4 .
|
-
- HY-W064657
-
|
|
JAK
|
Others
|
|
Momelotinib (dihydrochloride) is a JAK1/JAK2 inhibitor that also antagonizes ACVR1, leading to downregulation of Hepcidin expression and increased availability of iron for erythropoiesis. Momelotinib (dihydrochloride) can reduce transfusion burden and spleen enlargement caused by myelofibrosis, showing potential value in research and application within the field of myelofibrosis .
|
-
- HY-B0195
-
-
- HY-U00363
-
|
FK-480
|
Cholecystokinin Receptor
|
Endocrinology
|
|
CHEMBL333994 (FK-480) is a potent and orally active Cholecystokinin A receptor (CCK-A receptor) antagonist, with an IC50 of 0.67 nM. CHEMBL333994 selectively antagonizes peripheral CCK receptors. CHEMBL333994 increases CCK mRNA level. CHEMBL333994 can be used for research of chronic pancreatitis .
|
-
- HY-B0195A
-
|
MK-341 sodium; SB 252218 sodium
|
Prostaglandin Receptor
Angiotensin Receptor
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
Tranilast sodium (MK-341 sodium) acts as an anti-atopic agent. Tranilast suppresses production of prostaglandin D2 (PGD2, IC50= 0.1 mM). Tranilast sodium exhibits anti-inflammatory and immunomodulatory effects . Tranilast sodium antagonizes angiotensin II and inhibits its biological effects in vascular smooth muscle cells .
|
-
- HY-P1108A
-
|
|
CFTR
|
Others
|
|
Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B TFA antagonizes CRF2-mediated inhibition of gastric emptying .
|
-
- HY-18698
-
|
|
iGluR
|
Neurological Disease
|
|
L-701324 is a potent, orally active NMDA receptor antagonist that antagonizes the activity of the NMDA receptor by blocking its glycine B binding site. L-701324 binds with high affinity to rat brain membranes (IC50=2 nM). L-701324 has antidepressant activity .
|
-
- HY-129851
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
NTP42 is a thromboxane A2 (TXA2) receptor antagonist with an IC50 of 3.278 nM for antagonizing T prostanoid receptor (TP)- mediated [Ca 2+] mobilization following stimulation of cells with the alternative TP agonist U46619 . NTP42 can be used for the treatment of pulmonary arterial hypertension (PAH) .
|
-
- HY-P99653
-
|
VAY-736
|
TNF Receptor
|
Cancer
|
|
Ianalumab (VAY-736) is a human, decarboxylated antibody against BAFF-R. Ianalumab can block the interaction between BAFF and BAFF-R and antagonize the apoptosis protection mediated by BAFF. Ianalumab exerts antibody-dependent cytotoxic (ADCC), depending on effector cell activation mediated by immune receptor tyrosine activation motif (ITAM) .
|
-
- HY-12025
-
|
JNJ-26854165
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
Serdemetan (JNJ-26854165) is a potent anticancer agent with radiosensitizing activity. Serdemetan exhibits antiproliferative activity in various p53 wild-type tumor cells. Serdemetan also antagonizes the Mdm2-HIF1α axis leading to decreased levels of glycolytic enzymes .
|
-
- HY-N9404
-
|
|
Sodium Channel
|
Neurological Disease
|
|
6-Benzoylheteratisine is an Aconitum alkaloid with potential neuroprotective activity. 6-Benzoylheteratisine can antagonize tetrodotoxin, inhibit the increase of [Na +]i, [Ca 2+]i and glutamate release, and block sodium channels. 6-Benzoylheteratisine has an inhibitory effect on the neuronal activity underlying epileptiform burst discharge .
|
-
- HY-P2468
-
|
BADBH3 103-127 (human); BADBH3 (human)
|
Bcl-2 Family
|
Cancer
|
|
BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD, can antagonize the function of Bcl-xL. BAD (103-127) (human) is reported to have almost 800-fold higher affinity for Bcl-XL than the 16-mer peptide .
|
-
- HY-169867
-
|
7-Benzylidenenaltrexone
|
Opioid Receptor
|
Neurological Disease
|
|
BNTX (7-Benzylidenenaltrexone) is a selective δ1-opioid receptor antagonist. BNTX antagonizes the antisecretory actions of DPDPE (HY-P1334), Deltorphin 2 (HY-P1013), and DAMGO (HY-P0210) competitively. BNTX can be used for research of antinociception .
|
-
- HY-107519
-
|
|
iGluR
|
Neurological Disease
|
|
(R)-3,4-DCPG is an AMPA and NMDA antagonist with a Kd of 77 μM for AMPA. (R)-3,4-DCPG complete antagonizes the NMDA-induced depolarization at a concentration of 500 μM. (R)-3,4-DCPG exhibits a weak antagonistic effect on kainate-induced depolarizations .
|
-
- HY-P10571
-
|
|
Melanocortin Receptor
|
Endocrinology
|
|
GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC50=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R .
|
-
- HY-137888A
-
|
oATP trisodium salt
|
P2X Receptor
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
Oxidized ATP (oATP) trisodium salt is a broad-spectrum P2 receptor inhibitor. Oxidized ATP trisodium salt irreversibly antagonizes P2X7R activation. Oxidized ATP trisodium salt inhibits c-reactive protein (CRP)-induced NLRP3 inflammasome activation. Oxidized ATP trisodium salt can be used for research of atherosclerosis .
|
-
- HY-160706
-
|
|
Drug Derivative
|
Cardiovascular Disease
|
|
HHQ16 is an orally active derivative of Astragaloside IV (HY-N0431). HHQ16 effectively reverses infarction-induced hypertrophy and heart failure by targeted degrading lnc4012/lnc9456 and antagonizing their effects on G3BP2/NF-κB signaling .
|
-
- HY-P10392
-
|
|
β-catenin
Wnt
|
Cancer
|
|
aStAx-35R, a stapled peptide, antagonizes nuclear form of β-catenin and inhibits Wnt signaling. aStAx-35R inhibits competitively the binding of β-catenin to TCF4. aStAx-35R selectively induces growth inhibition of Wnt-dependent cancer cells .
|
-
- HY-14561A
-
|
RX 781094 hydrochloride
|
Adrenergic Receptor
Imidazoline Receptor
|
Neurological Disease
Endocrinology
|
|
Idazoxan hydrochloride (RX 781094 hydrochloride) is an α2-adrenoceptor antagonist and is also a imidazoline receptors (IRs) antagonist competitively antagonized the centrally induced hypotensive effect of imidazoline-like agents (IMs). Idazoxan hydrochloride also improves motor symptoms in Parkinson’s disease, L-DOPA-induced dyskinesias, and experimental Parkinsonism .
|
-
- HY-15064R
-
|
|
TRP Channel
|
Neurological Disease
|
|
HC-030031 (Standard) is the analytical standard of HC-030031. This product is intended for research and analytical applications. HC-030031 is a potent and selective TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.
|
-
- HY-148643
-
|
|
STING
|
Inflammation/Immunology
|
|
STING modulator-5 (compound 38) is a STING modulator with a pIC50 value of 9.5. STING modulator-5 antagonizes peripheral blood mononuclear cells (PBMC) with a pIC50 value of 8.1. STING modulator-5 is a antagonist of THP-1 cells, it can be used for immunological disease research .
|
-
- HY-146027
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 4 (Compound AT2) is an androgen receptor (AR) antagonist with an IC50 of 0.15 μM. Androgen receptor antagonist 4 efficiently antagonizes AR transcriptional activity, suppresses downstream target gene of AR, and blocks the DHT-induced AR nuclear translocation. Androgen receptor antagonist 4 shows anticancer activities .
|
-
- HY-118242
-
|
|
Estrogen Receptor/ERR
Calmodulin
|
Others
|
|
RU 45144 is an anti-estrogen compound that has the activity of antagonizing the binding of estrogen receptors to calmodulin. RU 45144 can inhibit the binding of estrogen receptors to calmodulin, and its effect is similar to that of tamoxifen. Its anti-estrogen effect may be related to specific side chains in the molecular structure, and the steroid skeleton may be involved in its anti-proliferative activity.
|
-
- HY-106684A
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Ridazolol hydrochloride is a β-adrenergic receptor (βAR) antagonist. Ridazolol hydrochloride exhibits a high degree of selectivity for β-1 adrenergic receptor (β1AR) and possesses moderate intrinsic sympathomimetic activity (ISA). Ridazolol hydrochloride can competitively antagonize the relaxation effects induced by isoproterenol. Ridazolol hydrochloride is utilized in the research of cardiovascular diseases .
|
-
- HY-126327
-
|
|
Histone Methyltransferase
|
Cancer
|
|
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
|
-
- HY-106684
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Ridazolol is a β-adrenergic receptor (βAR) antagonist. Ridazolol exhibits a high degree of selectivity for β-1 adrenergic receptor (β1AR) and possesses moderate intrinsic sympathomimetic activity (ISA). Ridazolol can competitively antagonize the relaxation effects induced by isoproterenol. Ridazolol is utilized in the research of cardiovascular diseases .
|
-
- HY-P0264
-
|
Avexitide
|
GLP Receptor
|
Metabolic Disease
|
|
Exendin(9-39) amide (Avexitide) is a glucagon-like peptide-1 (GLP-1) antagonist that competes with endogenous GLP-1 for binding to GLP-1 receptors, thereby antagonizing the effects of excess GLP-1 secretion. Exendin(9-39) amide can be used to study postoperative hypoglycemia (PBH) .
|
-
- HY-19432
-
|
|
iGluR
|
Neurological Disease
|
|
UBP-282 is a potent, selective and competitive AMPA and kainate receptor antagonist. UBP-282 inhibits the fast component of the dorsal root-evoked ventral root potential (fDR-VRP) with an IC50 value of 10.3 μM. UBP-282 antagonizes kainate-induced depolarisations of dorsal roots with a pA2 value of 4.96 .
|
-
- HY-100627A
-
|
|
MEK
|
Cancer
|
|
APS-2-79 hydrochloride is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATP biotin binding to KSR2 within the KSR2-MEK1 complexe with an IC50 of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling .
|
-
- HY-100627
-
|
|
MEK
|
Cancer
|
|
APS-2-79 is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATP biotin binding to KSR2 within the KSR2-MEK1 complexe with an IC50 of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling .
|
-
- HY-14939A
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Vapitadine hydrochloride (Compound 3a) is a selective, orally active and nonsedating antihistamine agent, which exhibits a good binding affinity with human cloned histamine H1 receptor with a Ki of 19 nM. Vapitadine hydrochloride decreases the histamine-induced lethality (ED50 is 0.056-1.2 mg/kg), antagonizes the cutaneous reactions to histamine (ED50 is 0.51-1.4 mg/kg) in rats .
|
-
- HY-149248
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
NF-κB-IN-8 competitively antagonizes LPS binding to MD-2. NF-κB-IN-8 reduces the expression of inflammatory factors by binding to MD-2. NF-κB-IN-8 also inhibits ALP activity. NF-κB-IN-8 can be used for the research of inflammation such as acute lung injury (ALI) .
|
-
- HY-101955
-
|
(2S,6S)-HNK hydrochloride
|
mTOR
nAChR
|
Neurological Disease
|
|
(2S,6S)-Hydroxynorketamine hydrochloride is a neurorelaxant with potential antidepressant and analgesic effects. (2S,6S)-Hydroxynorketamine hydrochloride can activate the mTOR pathway, increase the phosphorylation level of downstream targets, and antagonize α7-nicotinic acetylcholine receptor (nAChR) to exert neuroactive properties .
|
-
- HY-126327A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
|
-
- HY-157429
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
25N-N1-Nap (compound 16) is a β-arrestin-biased 5-HT2A agonist. 25N-N1-Nap antagonizes phencyclidine induced hyperactivity in Male C57BL/6 J mice .
|
-
- HY-19976
-
RN-1747
4 Publications Verification
|
TRP Channel
|
Cardiovascular Disease
|
|
RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 (TRPV4) agonist, with EC50 values are 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively. RN-1747 also antagonizes TRPM8, with an IC50 of 4 μM .
|
-
- HY-135046
-
|
|
DNA/RNA Synthesis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
MTOB sodium is a potent C-terminal binding protein (CtBP) inhibitor. MTOB sodium attenuates repetitive head injury-elicited neurologic dysfunction and neuroinflammation via inhibition of the transactivation activity of CtBP1 and CtBP2. MTOB sodium antagonizes the transcriptional regulatory activity of CtBP1 and CtBP2 by eviction from their target promoters in breast cancer cell lines .
|
-
- HY-123123
-
|
|
Prostaglandin Receptor
Endogenous Metabolite
|
Cardiovascular Disease
|
|
RS-61756-007 is a selective thromboxane receptor (TP) agonist with high activity at the TP receptor. RS-61756-007 showed agonism at TP and FP receptors in in vitro studies but had no activity at other receptor subtypes. The effects of RS-61756-007 can be antagonized in a similar manner by the TP antagonist SQ 29,548 .
|
-
- HY-147222
-
SAE-14
1 Publications Verification
GPR183 antagonist-1
|
EBI2/GPR183
|
Neurological Disease
Inflammation/Immunology
|
|
SAE-14 (compound SAE-14) is a potent, specific GPR183 antagonist with an IC50 value of 28.5 nM, can antagonize 7α, 25-OHC–induced calcium mobilization with IC50 value below 50 nM in HL-60 cells. GPR183 antagonist-1 can reverse allodynia in mice .
|
-
- HY-107518
-
|
(R,S)-3,4-DCPG
|
iGluR
|
Neurological Disease
|
|
(R,S)-3,4-Dicarboxyphenylglycine ((RS)-3,4-DCPG) is an AMPA receptor antagonist. (R,S)-3,4-Dicarboxyphenylglycine antagonizes AMPA-mediated depolarization of motor neurons in neonatal rats. (R,S)-3,4-Dicarboxyphenylglycine can be used in the study of neurological diseases .
|
-
- HY-12783
-
|
|
GABA Receptor
|
Neurological Disease
|
|
SCH 50911 hydrochloride, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC50 of 1.1 μM. SCH 50911 hydrochloride antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated 3H overflow with an IC50 of 3 μM.
|
-
- HY-157792
-
|
|
mAChR
|
Neurological Disease
|
Antidepressant agent 6 (S-3a) is a lead compound with potent and sustained antidepressant effects. Antidepressant agent 6 (S-3a) displays high cognitive safety margin.Antidepressant agent 6 (S-3a) antagonizes M1 receptors and elevates BDNF levels, suggesting its potential as an antidepressant for further exploration .
|
-
- HY-P10392B
-
|
|
β-catenin
Wnt
|
Cancer
|
|
aStAx-35R TFA, a stapled peptide, antagonizes nuclear form of β-catenin and inhibits Wnt signaling. aStAx-35R TFA inhibits competitively the binding of β-catenin to TCF4. aStAx-35R TFA selectively induces growth inhibition of Wnt-dependent cancer cells .
|
-
- HY-B0503
-
|
Thiouracil
|
NO Synthase
|
Endocrinology
Cancer
|
|
2-Thiouracil (Thiouracil) is a selective neuronal nitric oxide synthase (nNOS) inhibitor with a Ki value of 20 μM. 2-Thiouracil antagonizes BH4-induced nNOS dimerization. 2-Thiouracil is also an antithyroid compound and a highly specific melanoma detector. 2-Thiouracil stimulates the growth of pea and corn root segments .
|
-
- HY-P99653A
-
|
|
TNF Receptor
Apoptosis
|
Cancer
|
|
Ianalumab (FUT8-KO) is an anti-BAFF-R monoclonal antibody expressed by CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucose deficiency enhances the ADCC effect of the antibody. Ianalumab (FUT8-KO) can block the interaction between BAFF and BAFF-R and antagonize the apoptosis protection mediated by BAFF .
|
-
- HY-122964
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
URB447 is a peripherally restricted CB1 cannabinoid antagonist (IC50: 313 nM and 41 nM for rat CB1 and human CB2 receptor respectively ). URB447 lowers food intake and body-weight gain in mice without entering the brain or antagonizing central CB1-dependent responses. URB447 can be used for research of obesity .
|
-
- HY-14405
-
|
GW679769
|
Neurokinin Receptor
Cytochrome P450
|
Neurological Disease
|
|
Casopitant (GW679769) is a potent, selective, brain-penetrant and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant antagonizes the emetic effects of Substance P (HY-P0201). Casopitant is also a substrate and weak to moderate inhibitor of CYP3A4. Casopitant is indicated for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV) .
|
-
- HY-U00363A
-
|
(rac)-FK-480
|
Cholecystokinin Receptor
Drug Isomer
|
Inflammation/Immunology
|
|
(rac)-CHEMBL333994 is the racemate of CHEMBL333994 (HY-U00363). CHEMBL333994 is a potent and orally active Cholecystokinin A receptor (CCK-A receptor) antagonist, with an IC50 of 0.67 nM. CHEMBL333994 selectively antagonizes peripheral CCK receptors. CHEMBL333994 increases CCK mRNA level. CHEMBL333994 can be used for research of chronic pancreatitis .
|
-
- HY-121675
-
|
BOL-148; Bromolysergide
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
2-Bromo-LSD (BOL-148; Bromolysergide) is a Dopamine Receptor antagonist that directly affects dopamine neurons in the substantia nigra neostriatum. 2-Bromo-LSD increases the hydroxylation of tyrosine in striatum and antagonizes the decrease of Apomorphine-induced DOPA accumulation. 2-Bromo-LSD also blocks the 5-HT Receptor mediated DOPA formation .
|
-
- HY-118295
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Pyrimidine-indole hybrid is a compound that inhibits ciliogenesis and has the activity of antagonizing the Hedgehog signaling pathway by destabilizing microtubules. Pyrimidine-indole hybrid exerts its biological effects by inhibiting ciliogenesis and deconstructing the stable form of α-tubulin. Pyrimidine-indole hybrid has shown its unique mechanism of action in in vitro cell experiments and zebrafish embryo models, interfering with microtubule dynamics .
|
-
- HY-118190
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
AL 8810 methyl ester is a prostaglandin F(2α) analog and a prostaglandin F(2α) receptor agonist. Can competitively antagonize the effects of the FP receptor agonist Fluprostenol (HY-108560). AL 8810 methyl ester has no significant potency against TP, DP, EP(2), EP(4) receptor subtypes in cell lines .
|
-
- HY-12783A
-
|
|
GABA Receptor
|
Neurological Disease
|
|
SCH 50911, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC50 of 1.1 μM. SCH 50911 antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated 3H overflow with an IC50 of 3 μM .
|
-
- HY-16935R
-
|
|
TRP Channel
|
Neurological Disease
|
|
Mavatrep (Standard) is the analytical standard of Mavatrep. This product is intended for research and analytical applications. Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca2+ influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain .
|
-
- HY-P9952
-
|
LymphoStat B
|
TNF Receptor
CD20
|
Inflammation/Immunology
Cancer
|
|
Belimumab (LymphoStat B) is a humanized IgG1λ monoclonal antibody against B-lymphocyte stimulator (BLyS) protein. Belimumab antagonizes BLyS activity in autoimmune diseases and B-lymphocyte malignancies. Belimumab can be used for systemic lupus erythematosus (SLE) research . The component ratio of this product is Active ingredient: Excipients = 1:1.0-1:1.2.
|
-
- HY-W007511R
-
|
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
4-Methyl-1-pentanol is a volatile aroma component of red wine, which is often used in the production and blending of wine. 4-Methyl-1-pentanol can also be used as an alcohol antagonist to antagonize the effects of ethanol and 1-butanol on cell-cell adhesion, and is used in the study of fetal alcohol syndrome .
|
-
- HY-B0195R
-
-
- HY-W007511
-
|
Isohexanol; Isohexyl alcohol
|
Others
|
Neurological Disease
|
|
4-Methyl-1-pentanol is a volatile aroma component of red wine, which is often used in the production and blending of wine. 4-Methyl-1-pentanol can also be used as an alcohol antagonist to antagonize the effects of ethanol and 1-butanol on cell-cell adhesion, and is used in the study of fetal alcohol syndrome .
|
-
- HY-144347
-
|
|
CXCR
|
Infection
Cancer
|
|
HF51116 is a potent antagonist of CXCR4. HF51116 strongly antagonizes SDF-1α-induced cell migration, calcium mobilization, and CXCR4 internalization. HF51116 inhibits HIV-1 infection via CXCR4. HF51116 has the potential for the research of HIV-1 infection, hematopoietic stem cell mobilization, and cancer metastasis .
|
-
- HY-162495
-
|
|
CCR
|
Inflammation/Immunology
|
|
IDOR-1117-2520 is a potent and selective antagonist of CCR6. IDOR-1117-2520 antagonizes the CCL20-mediated calcium flow (IC50 = 63 nM) and inhibits β-arrestin recruitment to human CCR6 (IC50 = 30 nM) in cells expressing recombinant human CCR6. IDOR-1117-2520 can be used for research of autoimmune diseases .
|
-
- HY-N11420
-
|
|
Bacterial
Phytohormone
|
Others
|
|
Coronatine is a plant growth regulator that mimicks the jasmonic acid-isoleucine conjugate (JA-Ile), targets the jasmonic acid receptor COI1, activates the jasmonic acid signaling pathway, thereby inhibiting salicylic acid (SA)-dependent defense responses. Coronatine antagonizes the stomatal closure, induces plant cell necrosis and chlorosis, interfers with plant hormone balance, thereby promoting pathogen infection .
|
-
- HY-134807
-
|
|
P2X Receptor
5-HT Receptor
Autophagy
|
Cancer
|
|
Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7 .
|
-
- HY-B0002B
-
|
GR 38032; SN 307
|
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
- HY-15018A
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
SSR126768A free base is an orally active antagonist for oxytocin receptor, with Ki of 0.44 nM. SSR126768A free base is a tocolytic agent, that antagonizes the Oxytocin (HY-17571)-induced intracellular Ca 2+ increase and prostaglandin release in human uterine smooth muscle cells, inhibits thus the Oxytocin (HY-17571)-induced uterine contraction and delays parturition in pregnant rats in labor .
|
-
- HY-B0267CS
-
|
Aroxybutynin-d10
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
|
(R)-Oxybutynin-d10 (Aroxybutynin-d10) is deuterium labeled (R)-Oxybutynin. (R)-Oxybutynin (Aroxybutynin) is the racemic isomer of Oxybutynin and an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antispasmodic, antimuscarinic, and anticholinergic activities and competitively antagonizes carbachol-induced contractions. (R)-Oxybutynin can be used to study urinary incontinence caused by neurogenic bladder dysfunction .
|
-
- HY-101586A
-
|
Lu 25-109 maleate
|
mAChR
|
Neurological Disease
|
|
Alvameline (Lu 25-109) maleate is a partial agonist of M1 and an antagonist of M2/M3. Alvameline maleate competitively antagonizes contractions induced by ammonium chloride (HY-Y1269) and electrical field stimulation in human detrusor muscle, indicating its potential application in regulating bladder function. Additionally, alvameline maleate can improve cognitive function following traumatic brain injury in rats .
|
-
- HY-B2065
-
|
(-)-Scopolamine hydrochloride; Hyoscine hydrochloride
|
mAChR
5-HT Receptor
|
Neurological Disease
|
|
Scopolamine (Hyoscine) hydrochloride is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrochloride competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrochloride can induce cognitive and memory deficits in animals. Scopolamine hydrochloride can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .
|
-
- HY-B0002
-
|
GR 38032 hydrochloride; SN 307 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron (GR 38032; SN 307) hydrochloride is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron hydrochloride exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron hydrochloride can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
- HY-W010062R
-
|
|
Reference Standards
Cytochrome P450
Estrogen Receptor/ERR
Drug Derivative
|
Metabolic Disease
Cancer
|
|
4-Chlorophenylacetic acid (Standard) is the analytical standard of 4-Chlorophenylacetic acid. This product is intended for research and analytical applications. 4-Chlorophenylacetic acid is a halogenated phenylacetic acid derivative. 4-Chlorophenylacetic acid is a potent aromatase inhibitor and antagonizes estrogen signaling. 4-Chlorophenylacetic acid can provide carbon and energy for Pseudomonas sp. strain CBS3. 4-Chlorophenylacetic acid is effective against estrogen-induced mammary tumorigenesis .
|
-
- HY-101189B
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinity histamine H4 receptor antagonist, with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity .
|
-
- HY-P3245
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-N6018
-
|
|
Caspase
TNF Receptor
SOD
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
Cancer
|
|
Beta-Eudesmol has anticancer and anti-inflammatory activities. Beta-Eudesmol can induce apoptosis. Beta-Eudesmol is a neostigmine antagonist. Beta-Eudesmol can antagonize neostigmine-induced neuromuscular failure. Beta-Eudesmol can be used in the study of sepsis diseases. Beta-Eudesmol is a sesquiterpene-like compound that can be extracted from the rhizome of Atractylodes lancea .
|
-
- HY-110010
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Nafadotride is a dopamine D3 receptor antagonist. Nafadotrode regulates dopamine signaling primarily by antagonizing dopamine D3 receptors. The dopamine D3 receptor plays an important role in regulating emotion, motivation, reward, and certain motor functions. By blocking these receptors, Nafadotrode may affect neurotransmission processes associated with these functions. Nafadotrode can be used to explore the role of dopamine D3 receptors in various behavioral and neuropsychiatric disorders .
|
-
- HY-P1318
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
|
-
- HY-18660S
-
|
PER977-d8 tetrahydrochloride diacetate
|
Isotope-Labeled Compounds
Factor Xa
Thrombin
|
Cardiovascular Disease
|
|
Ciraparantag-d8 (PER977-d8) tetrahydrochloride diacetate is the deuterium labeled Ciraparantag (HY-18660). Ciraparantag is a thrombin and factor Xa inhibitor. Ciraparantag is a broad-spectrum reversal agent for anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants. It is reported to antagonize the effects of all coagulants except VKAs and agratroban .
|
-
- HY-N10534
-
|
Lewis X
|
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Lewis X trisaccharide (Lewis X, Le x) is a potent TH2 regulator, antagonizes LPS-induced IL-12 immune expression. Lewis X trisaccharide is a human histo-blood group antigen, plays an key role in cell-cell adhesion, and servers as a tumor marker. Lewis X trisaccharide is highly expressed in the outer membrane of the parasite, can be used for the immunology research of schistosomiasis .
|
-
- HY-P3245A
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-101222
-
|
|
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
SB-203186 hydrochloride is a potent, selective and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively .
|
-
- HY-126230A
-
|
|
Endogenous Metabolite
|
Cancer
|
|
(Rac)-PAT-494 is a type II autotaxin inhibitor with the activity of inhibiting the production of lysophosphatidic acid (LPA) in the blood. (Rac)-PAT-494 can participate in the inhibition of diseases related to cancer, fibrosis and inflammation by antagonizing the function of autotaxin. (Rac)-PAT-494 shows high activity in biochemical and plasma tests. (Rac)-PAT-494 can reduce plasma LPA levels after oral administration to rats .
|
-
- HY-P1318A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
|
-
- HY-121311
-
|
|
Serotonin Transporter
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Metrenperone is an inhibitor for 5-HT2 receptor. Metrenperone exhibits α1 and α2 antagonist activity as well as anti-H1 and anti-dopaminergic efficacy. Metrenperone can lower the blood pressure, enhances bradycardia in peripheral ischemia, inhibits serotonin-induced platelet aggregation, and antagonizes serotonin-mediated vasoconstriction. Metrenperone promotes the repair of acutely damaged collagen tissue .
|
-
- HY-14561AR
-
|
|
Adrenergic Receptor
Imidazoline Receptor
|
Neurological Disease
Endocrinology
|
|
Idazoxan (hydrochloride) (Standard) is the analytical standard of Idazoxan (hydrochloride). This product is intended for research and analytical applications. Idazoxan hydrochloride (RX 781094 hydrochloride) is an α2-adrenoceptor antagonist and is also a imidazoline receptors (IRs) antagonist competitively antagonized the centrally induced hypotensive effect of imidazoline-like agents (IMs). Idazoxan hydrochloride also improves motor symptoms in Parkinson’s disease, L-DOPA-induced dyskinesias, and experimental Parkinsonism .
|
-
- HY-B0281A
-
|
|
Histamine Receptor
|
Metabolic Disease
Cancer
|
|
Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine hydrochloride antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine hydrochloride inhibits breast tumor development and spread in mice .
|
-
- HY-102011
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation .
|
-
- HY-117005
-
|
|
Bacterial
|
Infection
|
|
C450-0730 is an antagonist targeting the AHL membrane-bound sensor kinase and is an antagonist of the nine-transmembrane protein LuxN of Vibrio harveyi . C450-0730 competitively binds to the LuxN AI-1 binding site and specifically antagonizes the LuxN/AI-1 quorum sensing signal in Vibrio harveyi. The inhibitory activity of C450-0730 against LuxN I209F was not significant .
|
-
- HY-101189
-
|
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
JNJ-39758979, a chemical probe, is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity .
|
-
- HY-115827
-
|
|
Prostaglandin Receptor
|
Others
|
|
AH22921 is an EP4 prostaglandin receptor antagonist with the activity of antagonizing the activation of adenylate cyclase by prostaglandins in CHO cells. AH22921 can shift the PGE2 concentration-response curve to the right in CHO cells. It is a non-competitive antagonist that is selective for EP4 receptors and has an antagonistic effect on EP4 receptors in CHO cells, but does not affect the PGE2 concentration-response curve in NPE cells containing EP2 receptors.
|
-
- HY-102011A
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
BMS-1166 hydrochloride is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 hydrochloride induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 hydrochloride antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation .
|
-
- HY-106194
-
|
|
Dopamine Receptor
Serotonin Transporter
|
Neurological Disease
|
|
SLV310 is an orally active dopamine D2 receptor antagonist (Ki: 5 nM) and serotonin reuptake receptor inhibitor. SLV310 antagonizes Apomorphine (HY-12723) induced climbing behaviour and 5-HTP (HY-N0122) induced serotonin syndrome like behaviour in mice (ED50: 5.6 and 5.9 mg/kg, p.o.). SLV310 is an antipsychotic compound and can be used for schizophrenia research .
|
-
- HY-114578
-
|
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
PD 118717 is a selective dopamine (DA) D-2 autoreceptor agonist. PD 118717 has significant affinity for 5-HT1A but not 5-HT1B and 5-HT2 receptors. PD 118717 is active in antagonizing the tau-Butyrolactone-induced accumulation of dopa in rat striatum and mesolimbic regions. PD 118717 exhibits an antipsychotic-like profile .
|
-
- HY-B0002A
-
|
GR 38032 hydrochloride dihydrate; SN 307 hydrochloride dihydrate
|
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron (GR 38032; SN 307) hydrochloride dehydrate is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron hydrochloride dehydrate exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron hydrochloride dehydrate can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
- HY-B0267B
-
|
Aroxybutynin hydrochloride
|
mAChR
|
Neurological Disease
|
|
(R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin hydrochloride has antimuscarinic, antispasmodic and anticholinergic activity, competitively antagonizes Carbachol-induced contractions. (R)-Oxybutynin hydrochloride can be used for researching incontinence due to neurogenic bladder dysfunction . (R)-Oxybutynin (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-B0693
-
|
|
Histamine Receptor
|
Metabolic Disease
Cancer
|
|
Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine inhibits breast tumor development and spread in mice .
|
-
- HY-18618A
-
|
|
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
SB-612111 hydrochloride hydrochloride is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 hydrochloride exhibits selectivity for μ-,?κ- and?δ-receptors with Ki values of?57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model .
|
-
- HY-12697
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
NGB 2904 is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 antagonizes Quinpirole-stimulated mitogenesis .
|
-
- HY-18618
-
|
|
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
SB-612111 is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model .
|
-
- HY-127024
-
|
|
Thyroid Hormone Receptor
|
Metabolic Disease
|
|
Thyroid hormone receptor antagonist (1-850) is a competitive, selective and high-affinity thyroid hormone receptor (TR) antagonist with an IC50 of 1.5 μM for antagonizing the effect of T3 on TR. Thyroid hormone receptor antagonist (1-850) blocks T3-mediated interaction of TRα and TRβ with nuclear receptor coactivator. Thyroid hormone receptor antagonist (1-850) has no effect on the activity of RARα .
|
-
- HY-18346
-
|
OPC-31260
|
Vasopressin Receptor
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
|
Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
|
-
- HY-176063
-
|
|
TRP Channel
Opioid Receptor
|
Neurological Disease
|
|
TRPV1 antagonist 11 (compound 2ac) is a potent TRPV1 antagonist with an IC50 of 29.3 nM. TRPV1 antagonist 11 is a potent μ-opioid receptor (MOR) agonist with a Ki of 60.3 nM. TRPV1 antagonist 11, a pyrimidine piperazine, exhibits pain relieving effects by antagonizing TRPV1 and stimulating MOR. TRPV1 antagonist 11 shows a potent, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice .
|
-
- HY-12697A
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
NGB 2904 hydrochloride is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 hydrochloride shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 hydrochloride antagonizes Quinpirole-stimulated mitogenesis .
|
-
- HY-W010892
-
|
Hyoscine hydrobromide trihydrate
|
mAChR
5-HT Receptor
|
Neurological Disease
|
|
Scopolamine (Hyoscine) hydrobromide trihydrate is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrobromide trihydrate competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrobromide trihydrate can induce cognitive and memory deficits in animals. Scopolamine hydrobromide trihydrate can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .
|
-
- HY-P0262
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Galantide, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide appears to bind to a single population of SP receptors (KD~40 nM) .
|
-
- HY-B1324A
-
|
Ro 13-8996 free base
|
Fungal
Cytochrome P450
Antibiotic
|
Infection
Cancer
|
|
Oxiconazole (Ro 13-8996) is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .
|
-
- HY-P991070
-
|
|
TNF Receptor
|
Cancer
|
|
ADG-106 is a fully human agonistic monoclonal IgG4 antibody against CD137 (4-1BB). ADG-106 has the mechanism to activate CD137 via strong FcγRIIB-mediated crosslinking while antagonizing CD137 ligands. The isotype control for ADG-106 can refer to Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
|
-
- HY-123593
-
|
OPC-31260 hydrochloride
|
Vasopressin Receptor
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
|
Mozavaptan hydrochloride (OPC-31260 hydrochloride) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan hydrochloride shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan hydrochloride has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
|
-
- HY-16935S
-
|
JNJ-39439335-d6
|
Isotope-Labeled Compounds
TRP Channel
|
Neurological Disease
|
|
Mavatrep-d6 (JNJ-39439335-d6) is a deuterated labeled Mavatrep (HY-16935). Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca 2+ influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain .
|
-
- HY-111283
-
|
(+)-AJ 76; (1S,2R)-AJ 76
|
Dopamine Receptor
|
Neurological Disease
|
|
AJ-76 ((+)-AJ 76; (1S,2R)-AJ 76) is a dopamine autoreceptor antagonist. AJ-76 can increase the synthesis and turnover of dopamine in the rat brain, while having little effect on the synthesis and turnover of serotonin (5-HT) and norepinephrine. AJ-76 can also antagonize the sedative effects of low-dose apomorphine and has a weak antagonistic effect on postsynaptic dopamine receptor .
|
-
- HY-A0081
-
|
|
Dopamine Receptor
SARS-CoV
Sodium Channel
|
Neurological Disease
Cancer
|
|
Fluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-107691
-
|
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects .
|
-
- HY-W010892S
-
|
Hyoscine-d3 hydrobromide
|
Isotope-Labeled Compounds
mAChR
5-HT Receptor
|
Neurological Disease
|
|
Scopolamine-d3 hydrobromide is the deuterium labeled Scopolamine hydrobromide (HY-B2065). Scopolamine (Hyoscine) hydrochloride is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrochloride competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrochloride can induce cognitive and memory deficits in animals. Scopolamine hydrochloride can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .
|
-
- HY-19279A
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
JTH-601 Free base is a novel alpha1-adrenoceptor antagonist that exhibits potent activity in inhibiting phenylephrine-induced contractions in lower urinary tract tissues. JTH-601 Free base competitively antagonizes alpha1-adrenoceptor-mediated contractile responses, demonstrating greater potency than prazosin or tamsulosin. JTH-601 Free base is anticipated to be effective in treating urinary outlet obstruction associated with benign prostatic hyperplasia.
|
-
- HY-119980B
-
|
|
Dopamine Receptor
Sodium Channel
SARS-CoV
|
Neurological Disease
Cancer
|
|
Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-121670
-
|
|
Others
|
Neurological Disease
|
|
Ambenoxan is a central nervous system-acting skeletal muscle relaxant that is effective in mice, rats, rabbits, dogs, and monkeys without loss of the righting reflex. It has no peripheral neuromuscular blocking effects and significantly reduces or eliminates decerebrate rigidity in rabbits, but does not antagonize the effects of strychnine, leptazol, or tremorine. Like other central nervous system depressants, ambenoxan prolongs sleep duration with hexobarbitone, but it has no local anesthetic effects. In anesthetized cats, the agent lowers blood pressure and reduces the pressor response to epinephrine, but has no effect on norepinephrine.
|
-
- HY-162759
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
Sigma-1 receptor antagonist 6 (Compound 12) is an antagonist of the Sigma-1 receptor (σ1R). Sigma-1 receptor antagonist 6 exerts a robust antiallodynic effect by antagonizing σ1R. Sigma-1 receptor antagonist 6 can be used in neuropathic pain animal models to alleviate mechanical allodynia induced by paclitaxel (HY-B0015) .
|
-
- HY-116790B
-
|
(Rac)-Penbutolol; (±)-Isopenbutolol
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
(±)-Penbutolol ((Rac)-Penbutolol) is the racemic mixture of Penbutolol. (±)-Penbutolol is an orally active β-adrenergic receptor antagonist. (±)-Penbutolol antagonizes exercise-induced tachycardia, reduces the increase in peak expiratory flow rate (PEFR) caused by exercise, and decreases resting plasma renin activity (PRA). (±)-Penbutolol reaches peak plasma concentration 1 hour after oral administration, with a half-life of 4.5 hours, and is converted into an active metabolite in the body. (±)-Penbutolol can be used in cardiovascular-related disease research .
|
-
- HY-119980
-
|
|
Sodium Channel
Dopamine Receptor
SARS-CoV
|
Infection
Neurological Disease
Cancer
|
|
Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-B1324
-
|
Ro 13-8996
|
Fungal
Cytochrome P450
Antibiotic
|
Infection
Cancer
|
|
Oxiconazole (Ro 13-8996) nitrate is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole nitrate is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole nitrate exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .
|
-
- HY-B1164A
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Bromopride hydrochloride is a selective, irreversible, competitive, and orally active dopamine D2 receptor antagonist. Bromopride hydrochloride can pass through the blood-brain barrier, inhibit the vomiting center, and enhance gastrointestinal motility, exerting antiemetic and gastrointestinal motility effects. Bromopride hydrochloride antagonizes dopamine-mediated vomiting reflexes and promotes gastrointestinal smooth muscle contraction, and has no adverse effects on abdominal wall healing in rats with postoperative abdominal infection. Bromopride hydrochloride can be used for the study of digestive system diseases (such as gastric hypomotility, nausea and vomiting) .
|
-
- HY-18617
-
|
|
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
rel-SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). rel-SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. rel-SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model .
|
-
- HY-P0039
-
|
|
Bombesin Receptor
|
Cancer
|
|
BIM-26226 is a selective gastrin-releasing peptide receptor (GRPR) (IC50 = 6 nM) and bombesin receptor (BN receptor) antagonist. BIM-26226 antagonizes BN- or GRP-stimulated amylase release with IC50 values of 0.3 nM and 0.2 nM, respectively. BIM-26226 is specific for the GRP-preferring BN receptor subtype with no interference with GRP receptor system. BIM-26226 can induce the synthesis of somatostatin receptor but has no significant effect on tumor growth .
|
-
- HY-P5756
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CSD-CH2(1,8)-NH2 is a selective and competitive KOR antagonist (Ki: 6.8 nM). CSD-CH2(1,8)-NH2 inhibits calcium mobilization in DRG neurons. CH2(1,8)-NH2 antagonizes the antinociceptive effect of U50,488. CSD-CH2(1,8)-NH2 can be used for research of neuropsychiatric disorders .
|
-
- HY-121670A
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
Ambenoxan hydrochloride is a central nervous system-acting skeletal muscle relaxant that is effective in mice, rats, rabbits, dogs, and monkeys without loss of the righting reflex. It has no peripheral neuromuscular blocking effects and significantly reduces or eliminates decerebrate rigidity in rabbits, but does not antagonize the effects of strychnine, leptazol, or tremorine. Like other central nervous system depressants, ambenoxan prolongs sleep duration with hexobarbitone, but it has no local anesthetic effects. In anesthetized cats, the agent lowers blood pressure and reduces the pressor response to epinephrine, but has no effect on norepinephrine.
|
-
- HY-N0546
-
|
Nuezhenoside
|
CaSR
RIP kinase
Mixed Lineage Kinase
TGF-beta/Smad
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Endocrinology
|
|
Ligustroflavone is an orally active flavonoid compound. Ligustroflavone can be extracted from Ligustrum lucidum. Ligustroflavone antagonizes the calcium-sensing receptor (CaSR), inhibits the RIPK1/RIPK3/MLKL pathway, and downregulates TGF-β/Smad signaling. Ligustroflavone regulates calcium metabolism, protects bone tissue, reduces cerebral ischemic injury, and inhibits liver fibrosis. Ligustroflavone can be used in the study of diabetic osteoporosis, ischemic stroke, and liver fibrosis .
|
-
- HY-108662
-
|
2,2'-Pyridylisatogen tosylate
|
P2Y Receptor
|
Inflammation/Immunology
Cancer
|
|
PIT (2,2'-Pyridylisatogen tosylate) is a selective and non-competitive antagonist of P2Y1 receptor with an IC50 value of 0.14 μM for human P2Y1 receptor. PIT antagonizes P2Y1 receptor signaling without affecting nucleotide binding. PIT is an irreversible antagonist of responses to ATP at metabotropic purinoceptors (of the P2Y family) in some smooth muscles. PIT can be used for the research of chronic bronchitis and asthma .
|
-
- HY-B1164
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Bromopride is a selective, irreversible, competitive, and orally effective dopamine D2 receptor antagonist. Bromopride can pass through the blood-brain barrier, inhibit the vomiting center, and enhance gastrointestinal motility, exerting antiemetic and gastrointestinal motility effects. Bromopride antagonizes dopamine-mediated vomiting reflexes and promotes gastrointestinal smooth muscle contraction, and has no adverse effects on abdominal wall healing in rats with postoperative abdominal infection. Bromopride can be used for the study of digestive system diseases (such as gastric hypomotility, nausea and vomiting) .
|
-
- HY-108531
-
|
|
RAR/RXR
|
Metabolic Disease
|
|
ER 50891 is a RARα antagonist. ER 50891 can significantly antagonize the inhibitory effect of all-trans retinoic acid (ATRA) on the total cell metabolic activity and proliferation of MC3T3-E1 preosteoblasts. ER 50891 rescues ATRA-inhibited osteocalcin (OCN) expression and extracellular matrix mineralization, and suppresses alkaline phosphatase (ALP) activity synergistically. ER 50891 can be used for the study of osteoporosis related to ATRA-induced inhibition of osteoblastogenesis .
|
-
- HY-108531A
-
|
|
RAR/RXR
|
Cancer
|
|
ER 50891 quarterhydrate is a RARα antagonist. ER 50891 can significantly antagonize the inhibitory effect of all-trans retinoic acid (ATRA) on the total cell metabolic activity and proliferation of MC3T3-E1 preosteoblasts. ER 50891 rescues ATRA-inhibited osteocalcin (OCN) expression and extracellular matrix mineralization, and suppresses alkaline phosphatase (ALP) activity synergistically. ER 50891 can be used for the study of osteoporosis related to ATRA-induced inhibition of osteoblastogenesis .
|
-
- HY-19057
-
|
MK-467; L-659066
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Vatinoxan (MK-467) is an alpha 2-adrenergic receptor antagonist. The peripheral selectivity of Vatinoxan determines that it has limited penetration across the blood-brain barrier and therefore has low concentrations in the central nervous system. Vatinoxan antagonizes alpha 2-adrenergic receptor receptors by binding to them, thereby reducing or preventing cardiovascular effects caused by α2-adrenergic agonists. Vatinoxan can be used in studies of cardiovascular effects, sedation and analgesia .
|
-
- HY-19858
-
|
|
iGluR
|
Neurological Disease
|
|
LY-466195 is a selective and competitive GLUK5 receptor antagonist. LY-466195 antagonizes Kainate-induced currents with an IC50 value of 0.045 μM in rat dorsal root ganglion neurons. In HEK293 cells transfected with GLUK5, GLUK2/GLUK5, or GLUK5/GLUK66 receptors, LY466195 produces IC50 values of 0.08 μM, 0.34 μM, and 0.07 μM, respectively .
|
-
- HY-118056
-
|
|
Cannabinoid Receptor
|
|
|
ABD459 is a CB1 receptor antagonist with significant effects on regulating food intake and sleep-wake cycles. ABD459 completely displaces CB1 agonist CP99540 (Ki = 8.6 nM) and antagonizes CP55940-induced GTPγS binding (KB = 7.7 nM). ABD459 may specifically modulate endogenous cannabinoid release through cholinergic activity and plays a role in attention and arousal regulation. ABD459 is suitable for research in neurological disorders .
|
-
- HY-13208
-
|
AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride
|
IAP
Apoptosis
|
Cancer
|
|
Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors .
|
-
- HY-13981
-
|
LGD-4033
|
Androgen Receptor
Apoptosis
Insulin Receptor
Caspase
|
Metabolic Disease
Endocrinology
|
|
Ligandrol is an orally active, selective androgen receptor (AR) agonist. Ligandrol enhances protein synthesis, inhibits muscle breakdown and oxidative stress, improves muscle cell viability and bone tissue microstructure, and reduces Cisplatin (HY-17394)-induced muscle toxicity and apoptosis. Ligandrol promotes muscle growth, protects bone structure, and has anti-diabetic, anti-apoptotic and antioxidant effects. Ligandrol can antagonize Streptozotocin (HY-13753) damage to pancreatic islets and improve the symptoms of type 2 diabetes .
|
-
- HY-121550
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
ME3221 is an angiotensin AT1 receptor antagonist that effectively antagonizes the pressor response to angiotensin II in rats and marmosets without affecting the hypotensive response to bradykinin. It demonstrates potent antihypertensive effects in renal hypertensive rats and spontaneously hypertensive rats (SHR), with efficacy comparable to or better than losartan in vivo. ME3221's repeated administration in SHR results in sustained and stable hypotensive effects without affecting heart rate, indicating its potential for treating both renal and essential hypertension similarly to losartan .
|
-
- HY-B0002BS1
-
|
GR 38032-d3; SN 307-d3
|
5-HT Receptor
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Ondansetron-d3 is the deuterium labeled Ondansetron (HY-B0002B ). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
- HY-118814
-
|
|
iGluR
|
Neurological Disease
|
|
YM928 is an orally active and noncompetitive α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist. YM928 inhibits AMPA receptor-mediated toxicity in primary rat hippocampal cultures with an IC50 value of 2 μM. YM928 blocks AMPA-induced intracellular calcium influx with an IC50 value of 3 μM and antagonizes AMPA-induced inward currents with an IC50 value of 1 μM. YM928 is promising for research of neurological disorders .
|
-
- HY-B2195
-
|
|
Adrenergic Receptor
|
Metabolic Disease
|
|
Aidioxa has the ability to improve delayed gastric emptying in rats. It can partially improve delayed gastric emptying caused by clonidine or restraint stress. The allyltoin part of Aidioxa restores gastric emptying activity by antagonizing α-2 adrenergic receptors. Its aluminum hydroxide part is involved in restoring gastric compliance. Aidioxa can improve both delayed gastric emptying and impaired gastric compliance, both of which play an important role in functional dyspepsia (FD). Aidioxa is a candidate agent for inhibiting FD.
|
-
- HY-B0281AS
-
|
|
Isotope-Labeled Compounds
Histamine Receptor
|
Metabolic Disease
Cancer
|
|
Ranitidine-d6 hydrochloride is the deuterium labeled Ranitidine hydrochloride (HY-B0281A) . Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine hydrochloride antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine hydrochloride inhibits breast tumor development and spread in mice .
|
-
- HY-170951
-
|
|
Androgen Receptor
|
Cancer
|
AR antagonist 10 (Compound Y5) is potent and orally active androgen receptor (AR) antagonist with an IC50 of 0.04 μM. AR antagonist 10 demonstrates dual mechanisms of action, antagonizes AR by disrupting AR dimerization, and induces AR degradation via the ubiquitin-proteasome pathway. AR antagonist 10 exhibits excellent activity against variant drug-resistant AR mutants. AR antagonist 10 effectively suppresses the tumor growth of the LNCaP xenograft. AR antagonist 10 is potential to be used for drug-resistant prostate cancer .
|
-
- HY-123468
-
|
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-120158
-
|
|
Potassium Channel
|
Neurological Disease
|
|
ZD0947 is an ATP-sensitive potassium channel activator with relatively effective activation of smooth muscle KATP channels (SUR2B/Kir6.1 and SUR2B/Kir6.2). ZD0947 partially antagonizes pancreatic KATP channels (SUR1/Kir6.2) and cardiac KATP channels (SUR2A/Kir6.2). ZD0947 is potentially used to inhibit overactive bladder (OAB) .
|
-
- HY-123468A
-
|
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
HA-1004 dihydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 dihydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 dihydrochloride is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-B0002BS
-
|
GR 38032-d5; SN 307-d5
|
5-HT Receptor
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Ondansetron-d5 is the deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
- HY-B0693S
-
|
|
Isotope-Labeled Compounds
Histamine Receptor
|
Cancer
|
|
Ranitidine-d6 is the deuterium labeled Ranitidine (HY-B0693). Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine inhibits breast tumor development and spread in mice .
|
-
- HY-B0002BR
-
|
GR 38032 (Standard); SN 307 (Standard)
|
Reference Standards
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Ondansetron (Standard) is the analytical standard of Ondansetron (HY-B0002B). This product is intended for research and analytical applications. Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
- HY-12927
-
|
|
CXCR
|
Inflammation/Immunology
|
|
SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca 2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model .
|
-
- HY-120985
-
|
|
Calcium Channel
|
Neurological Disease
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Xestospongins and araguspongins are marine natural products first isolated from Pacific basin sponges, and noted to have vasodilatory properties.1 Inositol phosphates (IP) are important signal transduction messengers acting via IP3 receptors to promote the mobilization of Ca2+ from intracellular stores.2 Araguspongin B antagonizes the calcium-releasing action of inositol 1,4,5-trisphosphate at the receptor level in cerebral microsomes, with an IC50 of 0.6 μM. It is nearly as potent as xestospongin C as an antagonist of the IP3 receptor.
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- HY-B0281AR
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Reference Standards
Histamine Receptor
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Metabolic Disease
Cancer
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Ranitidine hydrochloride (Standard) is the analytical standard of Ranitidine hydrochloride (HY-B0281A). This product is intended for research and analytical applications. Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine hydrochloride antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine hydrochloride inhibits breast tumor development and spread in mice.
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- HY-N2078
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Neodiosgenin
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LXR
Reactive Oxygen Species (ROS)
Apoptosis
Fatty Acid Synthase (FASN)
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Metabolic Disease
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Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes. Yamogenin is a steroidal saponin that can be obtained from plant species with in vitro cytotoxicity, antioxidant, and antimicrobial properties. Yamogenin induces cell death via the extrinsic and intrinsic way of apoptosis. Yamogenin inhibits protein denaturation with an IC50 of 1421.92 μg/mL. Yamogenin can be studied in research on gastric cancer .
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- HY-109139
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NIR178; PBF509
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Adenosine Receptor
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Neurological Disease
Cancer
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Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A2A receptor (A2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972). Taminadenant reactivate the antitumor immune response .
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- HY-123593R
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Vasopressin Receptor
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Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
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Mozavaptan (hydrochloride) (Standard) is the analytical standard of Mozavaptan (hydrochloride). This product is intended for research and analytical applications. Mozavaptan hydrochloride (OPC-31260 hydrochloride) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan hydrochloride shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan hydrochloride has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
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- HY-112348
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Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
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Cardiovascular Disease
Metabolic Disease
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HA-1004 hydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 hydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein (Cyclic GMP-AMP Synthase), and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 hydrochloride an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
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- HY-15543A
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5-HT Receptor
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Neurological Disease
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CP-809101 hydrochloride is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A receptor. CP-809101 hydrochloride inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 hydrochloride also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence .
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- HY-149434
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Androgen Receptor
PROTACs
Apoptosis
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Cancer
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PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule protein-targeting chimera (PROTACs) targeting the Androgen Receptor AR-V7. PROTAC AR-NTD antagonist 1 antagonizes the N-terminal domain of AR (AR-NTD), degrades AR-V7 protein, and induces apoptosis in prostate cancer (PC) cells. The efficiencies of PROTAC AR-NTD antagonist 1 in degrading AR-V7 in VCaP cells were 62.2% (1 μM) and 71.1% (5 μM), respectively .
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- HY-163345
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5-HT Receptor
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Neurological Disease
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5-HT7R antagonist 2 (compound 4h) is a 5-HT7R antagonist that antagonizes the G protein and β-arrestin signaling pathways, with a Ki of 67 nM, the IC50 values in cAMP and Tango tests were 2.59 μM and 39.57 μM, respectively. 5-HT7R antagonist 2 has an effect on neurogenesis and can reduce repetitive behaviors related to autism spectrum disorder (ASD) and restore neurogenesis of ASD impairment .
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- HY-18346R
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Vasopressin Receptor
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Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
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Mozavaptan (Standard) is the analytical standard of Mozavaptan. This product is intended for research and analytical applications. Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
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- HY-B0002BS2
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GR 38032-13C,d3; SN 307-13C,d3
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Isotope-Labeled Compounds
5-HT Receptor
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Neurological Disease
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Ondansetron- 13C,d3 is the 13C- and deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
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- HY-110206
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Cannabinoid Receptor
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Metabolic Disease
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AM6545 is a highly selective, brain-free (peripherally active) CB1 receptor antagonist (Ki=1.7 nM). AM6545 inhibits endocannabinoid signaling by competitively antagonizing CB1 receptors, inhibiting CB1-mediated appetite stimulation and inflammatory responses without affecting cAMP levels. AM6545 significantly reduces food intake and body weight in mice, while improving metabolic syndrome-related renal impairment (such as proteinuria, fibrosis) and insulin resistance. AM6545 can be used in the study of obesity and its complications .
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- HY-B0267BS
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mAChR
Isotope-Labeled Compounds
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Neurological Disease
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Oxybutynin-d5 hydrochloride is deuterated labeled (R)-Oxybutynin hydrochloride (HY-B0267B). (R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin hydrochloride has antimuscarinic, antispasmodic and anticholinergic activity, competitively antagonizes Carbachol-induced contractions. (R)-Oxybutynin hydrochloride can be used for researching incontinence due to neurogenic bladder dysfunction . (R)-Oxybutynin hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-134816
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Toll-like Receptor (TLR)
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Metabolic Disease
Inflammation/Immunology
Cancer
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D-Glucan is an orally effective Dectin-1 receptor immune activator with antioxidant properties (reducing TNF-α). D-Glucan activates macrophages and neutrophils to scavenge free radicals, inhibit oxidative stress and inflammatory responses, and improve insulin sensitivity. D-Glucan promotes glycolysis by enhancing the activity of the antioxidant enzyme glutathione, inhibiting gluconeogenesis and activating GK. D-Glucan can be used in the research of liver damage protection (antagonizing Acetaminophen (HY-66005) toxicity), radiation protection (synergistic with vitamin E) and diabetes (improving glucose metabolism) .
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- HY-119980BS
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Isotope-Labeled Compounds
Dopamine Receptor
Sodium Channel
SARS-CoV
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Neurological Disease
Cancer
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Fluphenazine-d6 (hydrochloride) is deuterium labeled Fluphenazine (hydrochloride). Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
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- HY-119980A
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Dopamine Receptor
Sodium Channel
SARS-CoV
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Infection
Neurological Disease
Cancer
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Fluphenazine dimaleate is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dimaleate blocks neuronal voltage-gated sodium channels. Fluphenazine dimaleate acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dimaleate can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dimaleate can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
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- HY-119980S
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Isotope-Labeled Compounds
Sodium Channel
Dopamine Receptor
SARS-CoV
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Others
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Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
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- HY-15543
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5-HT Receptor
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Neurological Disease
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CP-809101 is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A receptor. CP-809101 inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence .
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- HY-W010892R
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Hyoscine hydrobromide trihydrate (Standard)
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mAChR
Reference Standards
5-HT Receptor
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Neurological Disease
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Scopolamine hydrobromide trihydrate (Standard) is the analytical standard of Scopolamine hydrobromide trihydrate (HY-W010892). This product is intended for research and analytical applications. Scopolamine (Hyoscine) hydrobromide is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrobromide competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrobromide can induce cognitive and memory deficits in animals. Scopolamine hydrobromide can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .
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- HY-170525
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CD73
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Inflammation/Immunology
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CD73-IN-19 (Compound 4ab) is a CD73 inhibitor (with a 44% inhibition rate of CD73 enzymatic activity at 100 μM). CD73-IN-19 (at 10 μM and 100 μM) can completely antagonize the blockade of T cell proliferation induced by TCR (T cell receptor) triggering (which is induced by CD73 activity), and it can also inhibit the hA2A receptor activity in HEK-293 cells (Ki is 3.31 μM). CD73-IN-19 holds promise for research in the field of immune diseases .
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- HY-N0546R
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Nuezhenoside (Standard)
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Reference Standards
CaSR
RIP kinase
Mixed Lineage Kinase
TGF-beta/Smad
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Cardiovascular Disease
Neurological Disease
Metabolic Disease
Endocrinology
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Ligustroflavone (Standard) is the analytical standard of Ligustroflavone (HY-N0546). This product is intended for research and analytical applications. Ligustroflavone is an orally active flavonoid compound. Ligustroflavone can be extracted from Ligustrum lucidum. Ligustroflavone antagonizes the calcium-sensing receptor (CaSR), inhibits the RIPK1/RIPK3/MLKL pathway, and downregulates TGF-β/Smad signaling. Ligustroflavone regulates calcium metabolism, protects bone tissue, reduces cerebral ischemic injury, and inhibits liver fibrosis. Ligustroflavone can be used in the study of diabetic osteoporosis, ischemic stroke, and liver fibrosis .
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- HY-B1090
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Calcium Channel
Histamine Receptor
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Cardiovascular Disease
Endocrinology
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Cinnarizine is an orally active, effective and selective inhibitor of L-type calcium channel Cav1.3 with an IC50 of 1.5 μM (in vestibular hair cells). Cinnarizine can cross the blood-brain barrier and regulate calcium homeostasis and dopamine neurotransmission. Cinnarizine inhibits the influx of calcium ions into smooth muscle cells by blocking L-type calcium channels, thereby relaxing vascular smooth muscle, improving cerebral circulation and reducing blood viscosity, while antagonizing dopamine receptors. Cinnarizine can be used in the study of vestibular vertigo, Meniere's disease and cerebrovascular diseases .
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- HY-B1324R
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Ro 13-8996 (Standard)
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Reference Standards
Fungal
Cytochrome P450
Antibiotic
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Infection
Cancer
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Oxiconazole nitrate (Standard) is the analytical standard of Oxiconazole nitrate. This product is intended for research and analytical applications. Oxiconazole (Ro 13-8996) nitrate is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole nitrate is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole nitrate exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .
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- HY-A0081R
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Reference Standards
Dopamine Receptor
SARS-CoV
Sodium Channel
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Neurological Disease
Cancer
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Fluphenazine (dihydrochloride) (Standard) is the analytical standard of Fluphenazine (dihydrochloride). This product is intended for research and analytical applications. Fluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
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- HY-107664A
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Neurotensin Receptor
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Neurological Disease
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SR 142948 dihydrochloride is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders .
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- HY-19975
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TRP Channel
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Neurological Disease
Cancer
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RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM) . RN-1734 clearly decreases the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells .
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- HY-107664
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Neurotensin Receptor
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Neurological Disease
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SR 142948 is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders .
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- HY-18346S
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OPC-31260-d6
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Isotope-Labeled Compounds
Vasopressin Receptor
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Metabolic Disease
Endocrinology
Cancer
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Mozavaptan-d6 (OPC-31260-d6) is the deuterium labeled Mozavaptan. Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
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- HY-111077
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JAK
STAT
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Inflammation/Immunology
Cancer
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INCB16562 is an orally active and selective inhibitor against JAK1/2 markedly selective over JAK3. INCB16562 potently inhibits interleukin-6 (IL-6)-induced phosphorylation of STAT3. Additionally, INCB16562 inhibits the proliferation and survival of myeloma cells dependent on IL-6 for growth, as well as the IL-6–induced growth of primary bone marrow-derived plasma cells. INCB16562 antagonizes the growth of myeloma xenografts in mice with antitumor activity. INCB16562 is promising for research of multiple myeloma .
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- HY-149433
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Androgen Receptor
Apoptosis
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Cancer
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BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7. BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor) and induces apoptosis in PC cells. BWA-522 inhibits tumor growth in LNCaP xenograft model studies (60 mg/kg, po; TGI=76%). The efficiencies of BWA-522 in degrading AR-V7 and AR-FL were 77.3% (1 μM) and 72.0% (5 μM) in VCaP and LNCaP cells, respectively .
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- HY-107664B
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Neurotensin Receptor
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Neurological Disease
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SR 142948 TFA is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 TFA antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 TFA blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 TFA shows blood-brain permeability and can be used in study of psychiatric disorders .
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- HY-113438
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Drug Metabolite
Bcl-2 Family
Akt
Apoptosis
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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15(S)-HPETE is a precursor of 15(S)-HETE (HY-113336). 15(S)-HPETE is a product of Arachidonic acid (HY-109590) in the 15-lipoxygenase pathway. 15(S)-HPETE reduces Bcl-2, Akt, and phosphorylated Akt protein levels. 15(S)-HPETE induces Apoptosis. 15(S)-HPETE antagonizes the angiogenic effects of 15(S)-HETE. 15(S)-HPETE exhibits antitumor effects against chronic myeloid leukemia. 15(S)-HPETE can be used in adipose tissue explant studies .
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- HY-N2078R
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Neodiosgenin (Standard)
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Reference Standards
LXR
Apoptosis
Fatty Acid Synthase (FASN)
Reactive Oxygen Species (ROS)
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Metabolic Disease
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Yamogenin (Standard) is the analytical standard of Yamogenin. This product is intended for research and analytical applications. Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes. Yamogenin is a steroidal saponin that can be obtained from plant species with in vitro cytotoxicity, antioxidant, and antimicrobial properties. Yamogenin induces cell death via the extrinsic and intrinsic way of apoptosis. Yamogenin inhibits protein denaturation with an IC50 of 1421.92 μg/mL. Yamogenin can be studied in research on gastric cancer .
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- HY-115314
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LG 30435
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Histamine Receptor
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Inflammation/Immunology
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Mequitamium iodide (LG 30435) is an antihistamine drug with antiallergic and bronchodilatory activity. Mequitamium iodide can effectively antagonize airway contraction and inflammatory responses induced by histamine and antigens. Mequitamium iodide has nanomolar affinity for the H1 and smooth muscle receptors of histamine and mequitin. Mequitamium iodide, when administered in aerosol form, significantly inhibits histamine- and antigen-induced increases in airway pressure in allergic mice. Mequitamium iodide reduces antigen-induced eosinophil accumulation in the airways. Mequitamium iodide also exhibits inhibitory effects on PAF-induced platelet aggregation and bronchoconstriction, and can be used in the study of allergic diseases such as rhinitis and asthma .
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- HY-W740977
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Isohexanol-d7
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Isotope-Labeled Compounds
Biochemical Assay Reagents
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Neurological Disease
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4-Methyl-1-pentanol-d7 (Isohexanol-d7) is the deuterium labeled 4-Methyl-1-pentanol (HY-W007511). 4-Methyl-1-pentanol is a volatile aroma component of red wine, which is often used in the production and blending of wine. 4-Methyl-1-pentanol can also be used as an alcohol antagonist to antagonize the effects of ethanol and 1-butanol on cell-cell adhesion, and is used in the study of fetal alcohol syndrome .
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- HY-122197
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ML339
3 Publications Verification
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CXCR
Apelin Receptor (APJ)
Arrestin
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Cancer
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ML339 is a selective CXCR6 antagonist with an IC50 of 140 nM. ML339 antagonizes β-arrestin recruitment and cAMP signaling pathway of human CXCR6 receptor induced by CXCL16, with IC50 of 0.3 μM and 1.4 μM, respectively. ML339 shows weaker activity against the recruitment of β-arrestin in mouse CXCR6 receptors, with an IC50 of 18 μM. ML339 has no inhibitory effect on CXCR5，CXCR4，CXCR6 and apelin receptor (APJ), with IC50 >79 μM. ML339 has the potential to promote the development of prostate cancer research .
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- HY-U00237B
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Adrenergic Receptor
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Others
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L-771688 hydrochloride is a potent and highly selective α1A-adrenoceptor antagonist (Kd=43-90 pM). L-771688 hydrochloride is effective against cloned human, rat and dog α1A-adrenergic receptors. L-771688 exhibits high affinity (Ki ≤ 1 nM) and over 500-fold selectivity over the α1B and α1D isoforms. L-771688 potently antagonizes norepinephrine-induced responses at these receptors. Inhibits contractions induced by phenylephrine or A-61603 in rat, dog, human and monkey models .
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- HY-B0693A
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Histamine Receptor
SARS-CoV
Bacterial
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Infection
Metabolic Disease
Cancer
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Ranitidine bismuth citrate is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine bismuth citrate antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine bismuth citrate has selectivity for SARS-CoV-2-infected cells. Ranitidine bismuth citrate also has anti-Helicobacter pylori infection. Ranitidine bismuth citrate inhibits breast tumor development and spread in mice .
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- HY-P1320A
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Opioid Receptor
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Inflammation/Immunology
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[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2?binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
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![[Nphe1]Nociceptin(1-13)NH2 TFA](//file.medchemexpress.eu/product_pic/hy-p1320a.gif)
- HY-131187
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Ligands for Target Protein for PROTAC
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Cancer
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BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1 . BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation .
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- HY-P1320
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Opioid Receptor
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Inflammation/Immunology
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[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
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![[Nphe1]Nociceptin(1-13)NH2](//file.medchemexpress.eu/product_pic/hy-p1320.gif)
- HY-16639
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GPR35
Neurotensin Receptor
|
Neurological Disease
Endocrinology
|
|
ML314 is a potent, BBB-penetrant and β-arrestin biased molecule agonist of NTR1 (EC50 = 1.9 μM). ML314 shows good selectivity against NTR2 and GPR35, but does not stimulate Ca2+ mobilization. ML314 can attenuate amphetamine-like hyperlocomotion in dopamine transporter knockout mice. ML314 attenuates methamphetamine-associated hyperlocomotion and potentiates the psychostimulant inhibitory effects of a ghrelin antagonist in wild type mouse model. ML314 also acts as an allosteric enhancer of endogenous neurotensin. ML314 antagonizes G protein signaling. ML314 can be studied in research for methamphetamine abuse conditions .
|
-
- HY-W380450
-
|
Viloxazin; Emovit
|
5-HT Receptor
|
Neurological Disease
|
|
Viloxazine is a non-brain-penetrant, selective norepinephrine transporter (NET) inhibitor (IC50= 0.26 μM) and 5-HT receptor modulator. Viloxazine antagonizes 5-HT2B receptors (Ki=4.2 μM) and agonizes 5-HT2C receptors (EC50= 32 μM), respectively, and enhances 5-HT neurotransmission by modulating 5-HT2B/C receptors. Viloxazine also competitively inhibits NET from increasing NE and DA levels in the synaptic cleft, and can be used in the study of attention deficit hyperactivity disorder (ADHD) .
|
-
- HY-W380450R
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Viloxazine is a non-brain-penetrant, selective norepinephrine transporter (NET) inhibitor (IC50= 0.26 μM) and 5-HT receptor modulator. Viloxazine antagonizes 5-HT2B receptors (Ki=4.2 μM) and agonizes 5-HT2C receptors (EC50= 32 μM), respectively, and enhances 5-HT neurotransmission by modulating 5-HT2B/C receptors. Viloxazine also competitively inhibits NET from increasing NE and DA levels in the synaptic cleft, and can be used in the study of attention deficit hyperactivity disorder (ADHD) .
|
-
- HY-N3945
-
|
O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396
|
Phosphodiesterase (PDE)
Calcium Channel
MMP
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer .
|
-
- HY-159577
-
|
|
PI3K
mTOR
Akt
|
Cancer
|
|
Nic-15 (compound 4n) is an anti-constrictive agent used to antagonize the hypovascularity of pancreatic tumors. The hypovascularity allows cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop drug resistance. Nic-15 can regulate the PI3K/Akt/mTOR pathway and alleviate ER stress induced by Gemcitabine (HY-17026). Nic-15 can significantly inhibit the migration and colony formation of MIA PaCa-2 and PANC-1 pancreatic cancer cells. The combination of Nic-15 and Gemcitabine can effectively solve the problem of pancreatic tumor resistance. In an in vivo xenograft model, Nic-15 can significantly enhance the efficacy of Gemcitabine .
|
-
- HY-125784
-
|
Viloxazin hydrochloride; Emovit hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Viloxazine hydrochloride is a non-brain-penetrant, selective norepinephrine transporter (NET) inhibitor (IC50=0.26 μM) and 5-HT receptor modulator. Viloxazine antagonizes 5-HT2B receptors (Ki=4.2 μM) and agonizes 5-HT2C receptors (EC50=32 μM), respectively, and enhances 5-HT neurotransmission by modulating 5-HT2B/C receptors. Viloxazine also competitively inhibits NET from increasing NE and DA levels in the synaptic cleft, and can be used in the study of attention deficit hyperactivity disorder (ADHD) .
|
-
- HY-158426
-
2-APQC
1 Publications Verification
|
Sirtuin
|
Cardiovascular Disease
|
|
2-APQC is an orally active and selective agonist of Sirtuin-3 (SIRT3) (Kd=2.756 μM), antagonizes Isoproterenol/ISO (HY-B0468)-induced cytotoxicity. 2-APQC activates the SIRT3-PYCR1 axis to enhance mitochondrial proline metabolism and inhibit the ROS-p38MAPK pathway by inhibiting signaling pathways such as mTOR-p70S6K, JNK, and TGF-β/Smad3. 2-APQC also activates the AMPK-Parkin axis to alleviate myocardial hypertrophy and fibrosis and protect cardiac function. 2-APQC can be used in the study of heart failure .
|
-
- HY-144224S
-
|
|
Isotope-Labeled Compounds
Opioid Receptor
iGluR
MMP
PI3K
Akt
NF-κB
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Tianeptine-d6 hydrochloride is the deuterium labeled Tianeptine hydrochloride. Tianeptine hydrochloride is an atypical antidepressant. Tianeptine hydrochloride is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine hydrochloride is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine hydrochloride increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine hydrochloride exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine hydrochloride inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine hydrochloride can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.
|
-
- HY-90003A
-
|
|
Opioid Receptor
iGluR
MMP
PI3K
Akt
NF-κB
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Tianeptine sodium salt is an atypical antidepressant. Tianeptine sodium salt is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine sodium salt is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine sodium salt increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine sodium salt exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine sodium salt inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine sodium salt can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects .
|
-
- HY-W040129
-
|
|
DNA Alkylator/Crosslinker
DNA/RNA Synthesis
Apoptosis
Caspase
|
Infection
Neurological Disease
Cancer
|
|
Chromomycin A3 is an inhibitor that selectively binds to GC-rich DNA sequences. Chromomycin A3 targets the DNA minor groove after forming a dimer with Mg 2+. Chromomycin A3 inhibits DNA replication and transcription, blocks the binding of Sp1 transcription factor to target gene promoters, downregulates the expression of anti-apoptotic proteins such as FLIP, Mcl-1, and XIAP, and induces S-phase cycle arrest and caspase-dependent apoptosis in tumor cells. Chromomycin A3 can antagonize oxidative stress induced by glutathione depletion and neuronal apoptosis induced by Camptothecin (HY-15660). Chromomycin A3 can be used in basic research on malignant tumors such as cholangiocarcinoma, and is a potential chemosensitizer and GC-rich region probe .
|
-
- HY-90003
-
|
|
Opioid Receptor
iGluR
MMP
PI3K
Akt
NF-κB
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Tianeptine is an atypical antidepressant. Tianeptine is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. tianeptine increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects .
|
-
- HY-120377
-
|
|
HBV
|
Cancer
|
|
CYP1A1 inhibitor 8a is a compound that potently and selectively inhibits the CYP1A1 enzyme and has the potential to prevent cancer. CYP1A1 inhibitor 8a exhibits more than 10-fold selectivity for CYP1A1 and more than 100-fold selectivity over other enzymes in the CYP1 subfamily. CYP1A1 inhibitor 8a can effectively antagonize B[a]P-mediated activation of the aryl hydrocarbon receptor (AhR) in yeast cells and protect human cells from CYP1A1-mediated B[a]P toxicity. CYP1A1 inhibitor 8a has the potential to be developed as a cancer chemopreventive agent .
|
-
- HY-90003S
-
|
|
Isotope-Labeled Compounds
Opioid Receptor
iGluR
MMP
PI3K
Akt
NF-κB
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Tianeptine-d12 is a deuterated analog of Tianeptine (HY-90003).Tianeptine is an atypical antidepressant. Tianeptine is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.
|
-
- HY-90003AR
-
|
|
Reference Standards
Opioid Receptor
iGluR
MMP
PI3K
Akt
NF-κB
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Tianeptine sodium salt (Standard) is the analytical standard of Tianeptine sodium salt (HY-90003A). This product is intended for research and analytical applications. Tianeptine sodium salt is an atypical antidepressant. Tianeptine sodium salt is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine sodium salt is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine sodium salt increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine sodium salt exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine sodium salt inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine sodium salt can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.
|
-
- HY-12716
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
BRL-44408 is a selective adrenergic receptor antagonist of α2A/α2B AR. BRL-44408 can effectively antagonize the inhibitory effects of norepinephrine or adrenergic receptor agonist Clonidine (HY-12721) on K +-induced [3H]norepinephrine and [3H]5-hydroxytryptamine release. BRL-44408 has a higher affinity for human platelet membranes containing α2A-adrenoceptors than BRL-41992 and Imiloxan (HY-101337). BRL-44408 may affect the release of norepinephrine and 5-hydroxytryptamine through a mechanism mediated by α2A-adrenoceptors, and has a potential role in the regulation of neurotransmitter release .
|
-
- HY-P99395
-
|
JNJ 56022473; CSL 362
|
Interleukin Related
|
Cancer
|
|
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
|
-
- HY-W040129R
-
|
|
Reference Standards
Bacterial
Fungal
Apoptosis
Antibiotic
|
Infection
Neurological Disease
Cancer
|
|
Chromomycin A3 (Standard) is the analytical standard of Chromomycin A3 (HY-W040129). This product is intended for research and analytical applications. Chromomycin A3 is an inhibitor that selectively binds to GC-rich DNA sequences. Chromomycin A3 targets the DNA minor groove after forming a dimer with Mg 2+. Chromomycin A3 inhibits DNA replication and transcription, blocks the binding of Sp1 transcription factor to target gene promoters, downregulates the expression of anti-apoptotic proteins such as FLIP, Mcl-1, and XIAP, and induces S-phase cycle arrest and caspase-dependent apoptosis in tumor cells. Chromomycin A3 can antagonize oxidative stress induced by glutathione depletion and neuronal apoptosis induced by Camptothecin (HY-15660). Chromomycin A3 can be used in basic research on malignant tumors such as cholangiocarcinoma, and is a potential chemosensitizer and GC-rich region probe .
|
-
- HY-W097625
-
|
|
Toll-like Receptor (TLR)
MyD88
p38 MAPK
NF-κB
Heme Oxygenase (HO)
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
6-Methoxyflavone is an orally active methoxyflavone. 6-Methoxyflavone suppresses neuroinflammation in microglia through the inhibition of TLR4/MyD88/p38 MAPK/NF-κB dependent pathways and the activation of HO-1/NQO-1 signaling. 6-Methoxyflavone induces S-phase arrest through the CCNA2/CDK2/p21CIP1 signaling pathway in HeLa cells. 6-Methoxyflavone inhibits NFAT Translocation into the nucleus and suppresses T cell activation. 6-Methoxyflavone partially restores chronic ethanol-induced behavioral deficits in mice. 6-Methoxyflavone antagonizes chronic constriction injury and diabetes associated neuropathic nociception expression. 6-Methoxyflavone can be used for the study of cancer, inflammation and neurological diseases .
|
-
- HY-N3097R
-
-
- HY-N3097
-
-
- HY-B0527A
-
|
|
Serotonin Transporter
5-HT Receptor
mAChR
Histamine Receptor
Adrenergic Receptor
Trk Receptor
Sodium Channel
Potassium Channel
Dopamine Transporter
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
|
-
- HY-B0527
-
|
|
Serotonin Transporter
Trk Receptor
Sodium Channel
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
mAChR
Potassium Channel
Dopamine Transporter
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with Ki = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
|
-
- HY-B0527AS
-
|
|
Isotope-Labeled Compounds
Serotonin Transporter
5-HT Receptor
Histamine Receptor
mAChR
Adrenergic Receptor
Trk Receptor
Sodium Channel
Potassium Channel
Dopamine Transporter
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Amitriptyline-d6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
|
-
- HY-B0527AR
-
|
|
Reference Standards
Serotonin Transporter
5-HT Receptor
Histamine Receptor
mAChR
Adrenergic Receptor
Trk Receptor
Sodium Channel
Potassium Channel
Dopamine Transporter
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Amitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-D2259
-
|
|
Fluorescent Dyes/Probes
|
|
PFI-7 is a probe, which binds to human GID4 (KD is 79 nM), and antagonizes the binding of Pro/N-degrons. PFI-7 can be utilized in C-terminal to LisH (CTLH) complex research and development of targeted protein degradation .
|
| Cat. No. |
Product Name |
Type |
-
- HY-134816
-
|
|
Carbohydrates
|
|
D-Glucan is an orally effective Dectin-1 receptor immune activator with antioxidant properties (reducing TNF-α). D-Glucan activates macrophages and neutrophils to scavenge free radicals, inhibit oxidative stress and inflammatory responses, and improve insulin sensitivity. D-Glucan promotes glycolysis by enhancing the activity of the antioxidant enzyme glutathione, inhibiting gluconeogenesis and activating GK. D-Glucan can be used in the research of liver damage protection (antagonizing Acetaminophen (HY-66005) toxicity), radiation protection (synergistic with vitamin E) and diabetes (improving glucose metabolism) .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-135108
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
QWF Peptide (Compound 4a) is a substance P antagonist with an IC50 of 0.09 μM. QWF Peptide antagonizes the SP-induced contraction of isolated guinea pig trachea strips with an IC50 of 4.7 μM .
|
-
- HY-P1471
-
|
22-52-Adrenomedullin (human)
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (AM) (22-52), human, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist, and also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat .
|
-
- HY-P2499A
-
|
|
Bcl-2 Family
|
Cancer
|
|
BAD (103-127) (human), FAM-labeled TFA is a FAM-labeled human BAD (103-127) (HY-P2468). BAD (103-127) (human) TFA, the 25-mer Bad peptide, is derived from the BH3 domain of BAD and can antagonize the function of Bcl-xL .
|
-
- HY-P5061
-
-
- HY-P0300
-
|
|
Bcl-2 Family
|
Cancer
|
|
Bak BH3 is derived from the BH3 domain of Bak, can antagonize the function of Bcl-xL in cells.
|
-
- HY-P2052
-
|
|
Opioid Receptor
Neurokinin Receptor
|
Others
|
|
AWL 60 is a compound with SP antagonist and weak opioid agonist properties, which can antagonize SP-agonists in vitro and attenuate the decrease in blood pressure caused by SP-agonists in vivo.
|
-
- HY-P2579
-
-
- HY-P1721
-
|
|
Bradykinin Receptor
|
Cardiovascular Disease
|
|
NPC 17731 is a new bradykinin (BK) receptor antagonist. NPC 17731 antagonized both the contractile and relaxant responses caused by BK in longitudinal smooth muscle with IC50 of 23 and 29 nM, respectively .
|
-
- HY-P3853
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 87389 is a potent NK2 receptor antagonist. GR 87389 antagonized GA 64349-induced smooth muscle strips contractions in a competitive manner in the human detrusor, prostate and prostatic urethra .
|
-
- HY-P2436
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
L-659837 is a NK2 receptor antagonist, and can antagonize GR 64349 (HY-P1278)-induced contraction. L-659837 can be used for study of urinary bladder disorders .
|
-
- HY-P10619
-
-
- HY-P3765
-
|
|
Peptides
|
Cardiovascular Disease
|
|
Auriculin A is a synthetic atrial natriuretic factor (ANF) with hemodynamic effect. Auriculin A antagonizes renal vasoconstriction in the dog, and influences on arterial baroreflex control of heart rate, systemic blood pressure, and perfusion pressure in the hind limb (perfused at constant flow) in rabbits .
|
-
- HY-P1329
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .
|
-
- HY-P2429
-
|
|
Opioid Receptor
|
Others
|
|
N,N-Diallyl-Tyr-Aib-Aib-Phe-Leu is a compound that can antagonize the δ-opioid receptor and the action of [D-Pen2,D-Pen ] enkephalin in vivo. Its antagonistic effect can be verified by specific behavioral experiments.
|
-
- HY-P1329A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity .
|
-
- HY-P10631
-
|
|
HSP
|
Inflammation/Immunology
|
|
Gp96-II is a gp96-blocking peptide that antagonizes gp96-mediated LPS(HY-D1056)-induced cytokine production. Gp96-II can be utilized in research on inflammatory disease .
|
-
- HY-P1471A
-
|
22-52-Adrenomedullin (human) (TFA)
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. Adrenomedullin (AM) (22-52), human also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat .
|
-
- HY-P2499
-
|
|
Bcl-2 Family
|
Cancer
|
|
BAD (103-127) (human), FAM-labeled is a FAM-labeled human BAD (103-127) (HY-P2468). BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD and can antagonize the function of Bcl-xL .
|
-
- HY-P1108
-
|
|
CFTR
|
Others
|
|
Astressin 2B is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B antagonizes CRF2-mediated inhibition of gastric emptying .
|
-
- HY-P1108A
-
|
|
CFTR
|
Others
|
|
Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B TFA antagonizes CRF2-mediated inhibition of gastric emptying .
|
-
- HY-P2468
-
|
BADBH3 103-127 (human); BADBH3 (human)
|
Bcl-2 Family
|
Cancer
|
|
BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD, can antagonize the function of Bcl-xL. BAD (103-127) (human) is reported to have almost 800-fold higher affinity for Bcl-XL than the 16-mer peptide .
|
-
- HY-P10571
-
|
|
Melanocortin Receptor
|
Endocrinology
|
|
GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC50=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R .
|
-
- HY-P10392
-
|
|
β-catenin
Wnt
|
Cancer
|
|
aStAx-35R, a stapled peptide, antagonizes nuclear form of β-catenin and inhibits Wnt signaling. aStAx-35R inhibits competitively the binding of β-catenin to TCF4. aStAx-35R selectively induces growth inhibition of Wnt-dependent cancer cells .
|
-
- HY-126327
-
|
|
Histone Methyltransferase
|
Cancer
|
|
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
|
-
- HY-P0264
-
|
Avexitide
|
GLP Receptor
|
Metabolic Disease
|
|
Exendin(9-39) amide (Avexitide) is a glucagon-like peptide-1 (GLP-1) antagonist that competes with endogenous GLP-1 for binding to GLP-1 receptors, thereby antagonizing the effects of excess GLP-1 secretion. Exendin(9-39) amide can be used to study postoperative hypoglycemia (PBH) .
|
-
- HY-126327A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
|
-
- HY-P10392B
-
|
|
β-catenin
Wnt
|
Cancer
|
|
aStAx-35R TFA, a stapled peptide, antagonizes nuclear form of β-catenin and inhibits Wnt signaling. aStAx-35R TFA inhibits competitively the binding of β-catenin to TCF4. aStAx-35R TFA selectively induces growth inhibition of Wnt-dependent cancer cells .
|
-
- HY-P3245
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-P1318
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
|
-
- HY-P3245A
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-P1318A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
|
-
- HY-P0262
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Galantide, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide appears to bind to a single population of SP receptors (KD~40 nM) .
|
-
- HY-P0039
-
|
|
Bombesin Receptor
|
Cancer
|
|
BIM-26226 is a selective gastrin-releasing peptide receptor (GRPR) (IC50 = 6 nM) and bombesin receptor (BN receptor) antagonist. BIM-26226 antagonizes BN- or GRP-stimulated amylase release with IC50 values of 0.3 nM and 0.2 nM, respectively. BIM-26226 is specific for the GRP-preferring BN receptor subtype with no interference with GRP receptor system. BIM-26226 can induce the synthesis of somatostatin receptor but has no significant effect on tumor growth .
|
-
- HY-P5756
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CSD-CH2(1,8)-NH2 is a selective and competitive KOR antagonist (Ki: 6.8 nM). CSD-CH2(1,8)-NH2 inhibits calcium mobilization in DRG neurons. CH2(1,8)-NH2 antagonizes the antinociceptive effect of U50,488. CSD-CH2(1,8)-NH2 can be used for research of neuropsychiatric disorders .
|
-
- HY-P1320A
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2?binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
|
-
- HY-P1320
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99514
-
|
AGEN1884
|
CTLA-4
|
Cancer
|
|
Zalifrelimab (AGEN1884) is a fully human IgG1 monoclonal antibody targeting CTLA-4 (CTLA-4). Zalifrelimab antagonizes the inhibitory checkpoints of immune cell activation regulated by CTLA-4 signaling .
|
-
- HY-P99659
-
|
ANB 019
|
Interleukin Related
|
Inflammation/Immunology
|
|
Imsidolimab (ANB 019) is a high-affinity, humanized monoclonal antibody of anti-IL-36R. Imsidolimab antagonizes IL-36 cytokine signal transduction. Imsidolimab has potential application in generalized pustular psoriasis (GPP) and other inflammatory skin diseases .
|
-
- HY-P99653
-
|
VAY-736
|
TNF Receptor
|
Cancer
|
|
Ianalumab (VAY-736) is a human, decarboxylated antibody against BAFF-R. Ianalumab can block the interaction between BAFF and BAFF-R and antagonize the apoptosis protection mediated by BAFF. Ianalumab exerts antibody-dependent cytotoxic (ADCC), depending on effector cell activation mediated by immune receptor tyrosine activation motif (ITAM) .
|
-
- HY-P9952
-
|
LymphoStat B
|
TNF Receptor
CD20
|
Inflammation/Immunology
Cancer
|
|
Belimumab (LymphoStat B) is a humanized IgG1λ monoclonal antibody against B-lymphocyte stimulator (BLyS) protein. Belimumab antagonizes BLyS activity in autoimmune diseases and B-lymphocyte malignancies. Belimumab can be used for systemic lupus erythematosus (SLE) research . The component ratio of this product is Active ingredient: Excipients = 1:1.0-1:1.2.
|
-
- HY-P99395
-
|
JNJ 56022473; CSL 362
|
Interleukin Related
|
Cancer
|
|
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
|
-
- HY-P99653A
-
|
|
TNF Receptor
Apoptosis
|
Cancer
|
|
Ianalumab (FUT8-KO) is an anti-BAFF-R monoclonal antibody expressed by CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucose deficiency enhances the ADCC effect of the antibody. Ianalumab (FUT8-KO) can block the interaction between BAFF and BAFF-R and antagonize the apoptosis protection mediated by BAFF .
|
-
- HY-P991070
-
|
|
TNF Receptor
|
Cancer
|
|
ADG-106 is a fully human agonistic monoclonal IgG4 antibody against CD137 (4-1BB). ADG-106 has the mechanism to activate CD137 via strong FcγRIIB-mediated crosslinking while antagonizing CD137 ligands. The isotype control for ADG-106 can refer to Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0201
-
-
-
- HY-B0098
-
-
-
- HY-N0541
-
-
-
- HY-N2197
-
-
-
- HY-N3320
-
-
-
- HY-N0201R
-
-
-
- HY-N13994
-
-
-
- HY-N13997
-
-
-
- HY-N13999
-
-
-
- HY-N13996
-
-
-
- HY-W010062
-
|
|
Source classification
|
Drug Derivative
Cytochrome P450
Estrogen Receptor/ERR
|
|
4-Chlorophenylacetic acid is a halogenated phenylacetic acid derivative. 4-Chlorophenylacetic acid is a potent aromatase inhibitor and antagonizes estrogen signaling. 4-Chlorophenylacetic acid can provide carbon and energy for Pseudomonas sp. strain CBS3. 4-Chlorophenylacetic acid is effective against estrogen-induced mammary tumorigenesis .
|
-
-
- HY-N9404
-
-
-
- HY-W007511R
-
-
-
- HY-W007511
-
-
-
- HY-N11420
-
-
-
- HY-B2065
-
-
-
- HY-W010062R
-
|
|
Microorganisms
Source classification
|
Reference Standards
Cytochrome P450
Estrogen Receptor/ERR
Drug Derivative
|
|
4-Chlorophenylacetic acid (Standard) is the analytical standard of 4-Chlorophenylacetic acid. This product is intended for research and analytical applications. 4-Chlorophenylacetic acid is a halogenated phenylacetic acid derivative. 4-Chlorophenylacetic acid is a potent aromatase inhibitor and antagonizes estrogen signaling. 4-Chlorophenylacetic acid can provide carbon and energy for Pseudomonas sp. strain CBS3. 4-Chlorophenylacetic acid is effective against estrogen-induced mammary tumorigenesis .
|
-
-
- HY-N6018
-
-
-
- HY-N10534
-
-
-
- HY-W010892
-
|
Hyoscine hydrobromide trihydrate
|
Alkaloids
Structural Classification
Other Alkaloids
Source classification
Datura metel L.
Solanaceae
Plants
|
mAChR
5-HT Receptor
|
|
Scopolamine (Hyoscine) hydrobromide trihydrate is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrobromide trihydrate competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrobromide trihydrate can induce cognitive and memory deficits in animals. Scopolamine hydrobromide trihydrate can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .
|
-
-
- HY-N0546
-
-
-
- HY-N2078
-
-
-
- HY-W010892R
-
|
Hyoscine hydrobromide trihydrate (Standard)
|
Alkaloids
Structural Classification
Other Alkaloids
Source classification
Datura metel L.
Solanaceae
Plants
|
mAChR
Reference Standards
5-HT Receptor
|
|
Scopolamine hydrobromide trihydrate (Standard) is the analytical standard of Scopolamine hydrobromide trihydrate (HY-W010892). This product is intended for research and analytical applications. Scopolamine (Hyoscine) hydrobromide is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrobromide competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrobromide can induce cognitive and memory deficits in animals. Scopolamine hydrobromide can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .
|
-
-
- HY-N0546R
-
-
-
- HY-N2078R
-
|
Neodiosgenin (Standard)
|
Structural Classification
other families
Source classification
Plants
Steroids
|
Reference Standards
LXR
Apoptosis
Fatty Acid Synthase (FASN)
Reactive Oxygen Species (ROS)
|
|
Yamogenin (Standard) is the analytical standard of Yamogenin. This product is intended for research and analytical applications. Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes. Yamogenin is a steroidal saponin that can be obtained from plant species with in vitro cytotoxicity, antioxidant, and antimicrobial properties. Yamogenin induces cell death via the extrinsic and intrinsic way of apoptosis. Yamogenin inhibits protein denaturation with an IC50 of 1421.92 μg/mL. Yamogenin can be studied in research on gastric cancer .
|
-
-
- HY-N3945
-
|
O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396
|
Infection
Alkaloids
Structural Classification
other families
Classification of Application Fields
Source classification
Plants
Isoquinoline Alkaloids
Glaucium flavum
Inflammation/Immunology
Disease Research Fields
Papaveraceae
|
Phosphodiesterase (PDE)
Calcium Channel
MMP
NF-κB
|
|
Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer .
|
-
-
- HY-W040129
-
|
|
Microorganisms
Source classification
|
DNA Alkylator/Crosslinker
DNA/RNA Synthesis
Apoptosis
Caspase
|
|
Chromomycin A3 is an inhibitor that selectively binds to GC-rich DNA sequences. Chromomycin A3 targets the DNA minor groove after forming a dimer with Mg 2+. Chromomycin A3 inhibits DNA replication and transcription, blocks the binding of Sp1 transcription factor to target gene promoters, downregulates the expression of anti-apoptotic proteins such as FLIP, Mcl-1, and XIAP, and induces S-phase cycle arrest and caspase-dependent apoptosis in tumor cells. Chromomycin A3 can antagonize oxidative stress induced by glutathione depletion and neuronal apoptosis induced by Camptothecin (HY-15660). Chromomycin A3 can be used in basic research on malignant tumors such as cholangiocarcinoma, and is a potential chemosensitizer and GC-rich region probe .
|
-
-
- HY-W040129R
-
|
|
Microorganisms
Source classification
|
Reference Standards
Bacterial
Fungal
Apoptosis
Antibiotic
|
|
Chromomycin A3 (Standard) is the analytical standard of Chromomycin A3 (HY-W040129). This product is intended for research and analytical applications. Chromomycin A3 is an inhibitor that selectively binds to GC-rich DNA sequences. Chromomycin A3 targets the DNA minor groove after forming a dimer with Mg 2+. Chromomycin A3 inhibits DNA replication and transcription, blocks the binding of Sp1 transcription factor to target gene promoters, downregulates the expression of anti-apoptotic proteins such as FLIP, Mcl-1, and XIAP, and induces S-phase cycle arrest and caspase-dependent apoptosis in tumor cells. Chromomycin A3 can antagonize oxidative stress induced by glutathione depletion and neuronal apoptosis induced by Camptothecin (HY-15660). Chromomycin A3 can be used in basic research on malignant tumors such as cholangiocarcinoma, and is a potential chemosensitizer and GC-rich region probe .
|
-
-
- HY-W097625
-
|
|
Structural Classification
Flavonoids
Flavones
Thymelaeaceae
Source classification
Plants
Pimelea simplex F.Muell.
|
Toll-like Receptor (TLR)
MyD88
p38 MAPK
NF-κB
Heme Oxygenase (HO)
|
|
6-Methoxyflavone is an orally active methoxyflavone. 6-Methoxyflavone suppresses neuroinflammation in microglia through the inhibition of TLR4/MyD88/p38 MAPK/NF-κB dependent pathways and the activation of HO-1/NQO-1 signaling. 6-Methoxyflavone induces S-phase arrest through the CCNA2/CDK2/p21CIP1 signaling pathway in HeLa cells. 6-Methoxyflavone inhibits NFAT Translocation into the nucleus and suppresses T cell activation. 6-Methoxyflavone partially restores chronic ethanol-induced behavioral deficits in mice. 6-Methoxyflavone antagonizes chronic constriction injury and diabetes associated neuropathic nociception expression. 6-Methoxyflavone can be used for the study of cancer, inflammation and neurological diseases .
|
-
-
- HY-N3097R
-
-
-
- HY-N3097
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-W010892S
-
|
|
|
Scopolamine-d3 hydrobromide is the deuterium labeled Scopolamine hydrobromide (HY-B2065). Scopolamine (Hyoscine) hydrochloride is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrochloride competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrochloride can induce cognitive and memory deficits in animals. Scopolamine hydrochloride can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .
|
-
-
- HY-B0281AS
-
|
|
|
Ranitidine-d6 hydrochloride is the deuterium labeled Ranitidine hydrochloride (HY-B0281A) . Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine hydrochloride antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine hydrochloride inhibits breast tumor development and spread in mice .
|
-
-
- HY-B0002BS
-
|
|
|
Ondansetron-d5 is the deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
-
- HY-B0098S
-
|
|
|
Doxazosin-d8 is a deuterium labeled Doxazosin (UK 33274). Doxazosin is a quinazoline-derivative that selectively antagonizes postsynaptic α1 adrenergic receptors .
|
-
-
- HY-B0745S
-
|
|
|
Ramatroban-d4 is deuterium labeled Ramatroban. Ramatroban is a selective thromboxane A2 (TxA2, IC50=14 nM) antagonist, which also antagonizes CRTH2 (IC50=113 nM) by inhibiting PGD2 binding.
|
-
-
- HY-B0267CS
-
|
|
|
(R)-Oxybutynin-d10 (Aroxybutynin-d10) is deuterium labeled (R)-Oxybutynin. (R)-Oxybutynin (Aroxybutynin) is the racemic isomer of Oxybutynin and an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antispasmodic, antimuscarinic, and anticholinergic activities and competitively antagonizes carbachol-induced contractions. (R)-Oxybutynin can be used to study urinary incontinence caused by neurogenic bladder dysfunction .
|
-
-
- HY-18660S
-
|
|
|
Ciraparantag-d8 (PER977-d8) tetrahydrochloride diacetate is the deuterium labeled Ciraparantag (HY-18660). Ciraparantag is a thrombin and factor Xa inhibitor. Ciraparantag is a broad-spectrum reversal agent for anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants. It is reported to antagonize the effects of all coagulants except VKAs and agratroban .
|
-
-
- HY-16935S
-
|
|
|
Mavatrep-d6 (JNJ-39439335-d6) is a deuterated labeled Mavatrep (HY-16935). Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca 2+ influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain .
|
-
-
- HY-B0002BS1
-
|
|
|
Ondansetron-d3 is the deuterium labeled Ondansetron (HY-B0002B ). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
-
- HY-B0693S
-
|
|
|
Ranitidine-d6 is the deuterium labeled Ranitidine (HY-B0693). Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine inhibits breast tumor development and spread in mice .
|
-
-
- HY-B0002BS2
-
|
|
|
Ondansetron- 13C,d3 is the 13C- and deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
|
-
-
- HY-B0267BS
-
|
|
|
Oxybutynin-d5 hydrochloride is deuterated labeled (R)-Oxybutynin hydrochloride (HY-B0267B). (R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin hydrochloride has antimuscarinic, antispasmodic and anticholinergic activity, competitively antagonizes Carbachol-induced contractions. (R)-Oxybutynin hydrochloride can be used for researching incontinence due to neurogenic bladder dysfunction . (R)-Oxybutynin hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
-
- HY-119980BS
-
|
|
|
Fluphenazine-d6 (hydrochloride) is deuterium labeled Fluphenazine (hydrochloride). Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
-
- HY-119980S
-
|
|
|
Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
-
- HY-18346S
-
|
|
|
Mozavaptan-d6 (OPC-31260-d6) is the deuterium labeled Mozavaptan. Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
|
-
-
- HY-W740977
-
|
|
|
4-Methyl-1-pentanol-d7 (Isohexanol-d7) is the deuterium labeled 4-Methyl-1-pentanol (HY-W007511). 4-Methyl-1-pentanol is a volatile aroma component of red wine, which is often used in the production and blending of wine. 4-Methyl-1-pentanol can also be used as an alcohol antagonist to antagonize the effects of ethanol and 1-butanol on cell-cell adhesion, and is used in the study of fetal alcohol syndrome .
|
-
-
- HY-144224S
-
|
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Tianeptine-d6 hydrochloride is the deuterium labeled Tianeptine hydrochloride. Tianeptine hydrochloride is an atypical antidepressant. Tianeptine hydrochloride is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine hydrochloride is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine hydrochloride increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine hydrochloride exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine hydrochloride inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine hydrochloride can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.
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- HY-90003S
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Tianeptine-d12 is a deuterated analog of Tianeptine (HY-90003).Tianeptine is an atypical antidepressant. Tianeptine is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.
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- HY-B0527AS
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Amitriptyline-d6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
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- HY-148695B
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Aptamers
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ADR58 sodium is a highly potent and selective human oncostatin M (OSM) antagonist, which can prevent the binding of OSM to the gp130 receptor and specifically antagonize OSM-mediated signaling. ADR58 sodium can be used in the research of rheumatoid arthritis related diseases .
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- HY-148695C
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Aptamers
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ADR58 sodium is a highly potent and selective human oncostatin M (OSM) antagonist, which can prevent the binding of OSM to the gp130 receptor and specifically antagonize OSM-mediated signaling. ADR58 sodium can be used in the research of rheumatoid arthritis related diseases .
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