Search Result
Results for "
blockade
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-P99540
-
PSB-205; QL1706 (iparomlimab/tuvonralimab); PBS105
|
PD-1/PD-L1
CTLA-4
|
Cancer
|
Tuvonralimab (PSB-205; QL1706) is a dual immune checkpoint blockade containing a mixture of anti-PD-1 IgG4 and anti-CTLA-4 IgG1 antibodies, Iparomlimab and Tuvonralimab .
|
-
-
- HY-W158030
-
2GBI
|
NOD-like Receptor (NLR)
|
Cancer
|
2-Guanidinobezimidazole is a selective agonist of NLRP3, with a KD value of 1.29 μM to His-GFP-NLRP3. 2-Guanidinobezimidazole binds directly to the LRR domain of NLRP3, promoting inflammasome assembly and activation. 2-Guanidinobezimidazole promotes anti-tumor immunity, inhibits tumor growth, and overcome immune checkpoint blockade (ICB) resistance .
|
-
-
- HY-B0292A
-
BW-33A
|
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Atracurium (BW-33A) besylate is a potent, competitive and non-depolarizing neuromuscular blocking agent. Atracurium besylate also is an AChR receptor antagonist. Atracurium besylate induces bronchoconstriction and neuromuscular blockade. Atracurium besylate promotes astroglial differentiation .
|
-
-
- HY-144501
-
|
Toll-like Receptor (TLR)
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
D18 is an immune modulator. D18 acts as a TLR7/8 dual agonist (EC50=24 nM for hTLR7 and 10 nM for hTLR8, respectively). D18 increases PD-L1 expression through epigenetic regulation, thus sensitizing tumors to PD-1/PD-L1 blockade. D18 is a ADC cytotoxin uesd for the systhesis of ADC HE-S2 .
|
-
-
- HY-153544
-
|
Toll-like Receptor (TLR)
|
Cancer
|
TLR7/8 agonist 9 (Compound 25a) is a TLR7/8 agonist, with EC50s of 40 nM and 23 nM for hTLR7/8. TLR7/8 agonist 9 has anti-tumor activity and improves the antitumor activity of PD-1/PD-L1 blockade. TLR7/8 agonist 9 can be used for research of cancer immunotherapy .
|
-
-
- HY-124047
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
RX 67668 is a potent cholinesterase inhibitor with an IC50 of 5 μM for both acetylcholinesterase (AChE) and butyrylcholinesterase. RX 67668 can reverse the neuromuscular blockade induced by D-tubocurarine. RX 67668 is a muscle relaxant used to relieve skeletal muscle fatigue .
|
-
-
- HY-B0292
-
BW-33A free acid
|
nAChR
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
tracurium (BW-33A free acid) is a potent, competitive and non-depolarizing neuromuscular blocking agent.Atracurium also is an AChR receptor antagonist. Atracurium induces bronchoconstriction and neuromuscular blockade. Atracurium promotes astroglial differentiation .
|
-
-
- HY-B0292AR
-
|
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Atracurium (besylate) (Standard) is the analytical standard of Atracurium (besylate). This product is intended for research and analytical applications. Atracurium (BW-33A) besylate is a potent, competitive and non-depolarizing neuromuscular blocking agent. Atracurium besylate also is an AChR receptor antagonist. Atracurium besylate induces bronchoconstriction and neuromuscular blockade. Atracurium besylate promotes astroglial differentiation .
|
-
-
- HY-163844
-
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
PD-1/PD-L1-IN-49 (compound 1c) is a potent inhibitor of PD-1/PD-L1, with the IC50 of 77 nM. PD-1/PD-L1-IN-49 activates Jurkat T cells, reflecting successful blockade of the PD-1/PD-L1 immune checkpoint .
|
-
-
- HY-135004
-
|
Adrenergic Receptor
|
Endocrinology
|
Su-4029 is an agent that interacts with alpha receptors. It negates the blockade of norepinephrine by the reversible adrenergic blocker phentolamine but not by the irreversible blocker Dibenamine, suggesting Su-4029 acts at the same site as these blockers. Su-4029 pretreatment results in three categories of responses to pressor phenylalkylamines: irreversible blockade of amines with no or only p-hydroxylation, reversible blockade of amines with beta-carbon hydroxylation, and no blockade or augmentation of amines with m and p-hydroxylation or m or p plus beta-hydroxylation. Su-4029 may deform the alpha receptor site affected by adrenergic blocking agents .
|
-
-
- HY-129254
-
-
-
- HY-121276
-
|
Dopamine Receptor
|
Neurological Disease
|
Benperidol is a relatively old antipsychotic agent. Benperidol is a butyrophenone antipsychotic, with the highest neuroleptic potency in terms of D2 receptor blockade .
|
-
-
- HY-116738
-
|
Others
|
Neurological Disease
|
Trimecaine, a local neural blockade agent, has a strong depressant effect on the cerebral cortex and the ascending reticular formation of the brain stem .
|
-
-
- HY-101809A
-
|
iGluR
|
Cardiovascular Disease
|
CNS-5161 is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
|
-
-
- HY-101809
-
CNS 5161A
|
iGluR
|
Cardiovascular Disease
|
CNS-5161 hydrochloride is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
|
-
-
- HY-P0142
-
|
PKG
|
Cardiovascular Disease
|
DT-3 is a membrane-permeable protein kinase G Iα (PKG Iα) inhibitory peptide and shows pharmacological blockade of the cGMP-PKG signalling .
|
-
-
- HY-108594
-
|
Potassium Channel
|
Metabolic Disease
|
PD-118057 is a hERG channel activator without causing hERG blockade. PD-118057 activates hERG channel to suppress changes in membrane excitability .
|
-
-
- HY-P0142A
-
|
PKG
|
Cardiovascular Disease
|
DT-3 acetate is a membrane-permeable protein kinase G Iα (PKG Iα) inhibitory peptide and shows pharmacological blockade of the cGMP-PKG signalling .
|
-
-
- HY-107728
-
-
-
- HY-107697
-
|
iGluR
|
Neurological Disease
|
N20C hydrochloride is a selective and noncompetitive open NMDA receptor open channel blocker, with micromolar affinity, fast on-off blockade kinetics, and strong voltage dependence. Neuroprotective activity .
|
-
-
- HY-152156
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis .
|
-
-
- HY-105084A
-
|
Sodium Channel
|
Neurological Disease
|
Lubeluzole (dihydrochloride) is a neuroprotective agent which blockades neuronal voltage-gated sodium channels. Lubeluzole (dihydrochloride) also produces both tonic and block of cardiac sodium channels. Lubeluzole (dihydrochloride) is promising for research of antiarrhythmic agents .
|
-
-
- HY-141549
-
|
Others
|
Inflammation/Immunology
|
BPK-21, an active acrylamide, suppresses T cell activation through blockade of ERCC3 function. BPK-21 specifically targets C342 in the helicase ERCC3 .
|
-
-
- HY-126635
-
|
Dopamine Receptor
Adrenergic Receptor
|
Others
|
Mafoprazine is a phenylpiperazine derivative with variable affinities for neuronal receptors. It may exert its antipsychotic effects primarily through D2 receptor blockade and α-adrenergic activity, and may increase the activity of dopamine metabolites.
|
-
-
- HY-121276R
-
|
Dopamine Receptor
|
Neurological Disease
|
Benperidol (Standard) is the analytical standard of Benperidol. This product is intended for research and analytical applications. Benperidol is a relatively old antipsychotic agent. Benperidol is a butyrophenone antipsychotic, with the highest neuroleptic potency in terms of D2 receptor blockade .
|
-
-
- HY-14408
-
|
Adenosine Receptor
|
Neurological Disease
|
Lu AA47070 is a phosphonooxymethylene prodrug of a potent and selective Adenosine A2A receptor antagonist. Lu AA47070 reverses the motor and motivational effects produced by dopamine D2 receptor blockade .
|
-
-
- HY-155847
-
|
Phosphatase
|
Cancer
|
LYP-IN-3 (compound D34) is a selective inhibitor of Lymphoid-tyrosine phosphatase (LYP) (Ki=0.93 μM), and regulates T-cell receptor (TCR) signaling pathway in tumor progress. LYP-IN-3 activates T-cell and inhibits M2 macrophage polarization, but upregulates PD-1/PD-L1 expression. LYP-IN-3 can be leveraged with PD-1/PD-L1 inhibitor, for futher cancer immunotherapy .
|
-
-
- HY-N2412
-
|
Chloride Channel
|
Neurological Disease
Cancer
|
Irisolidone is a major isoflavone found in Pueraria lobata flowers. Irisolidone exhibits potent hepatoprotective activity. Irisolidone shows the high efficacy for volume-regulated anion channels (VRAC) blockade (IC50=9.8 μM) .
|
-
-
- HY-B0423
-
Eustigmin bromide; Neoserine bromide
|
Cholinesterase (ChE)
|
Neurological Disease
|
Neostigmine (Eustigmin) Bromide is an orally active and reversible cholinesterase inhibitor that acts on myasthenia gravis to prolong and intensify the muscarinic and nicotinic effects of acetylcholine. Neostigmine Bromide can be used in anesthesia to reverse the neuromuscular blockade produced by competitive neuromuscular blockers .
|
-
-
- HY-14828
-
SMP-986
|
mAChR
|
Metabolic Disease
|
Afacifenacin (SMP-986) is a potent and orally active muscarinic receptor antagonist. Afacifenacin inhibits the bladder afferent pathway through the sodium-channel blockade, increasing volume, and reducing the frequency of urination and incontinence. Afacifenacin has the potential for the research of overactive bladder (OAB) .
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-
-
- HY-172348
-
|
Antibiotic
|
Infection
|
BRD-9327 is an inhibitor of EfpA. BRD-9327 binds in the outer vestibule without complete blockade of the substrate path to the outside, suggesting its possible inhibition of the movement necessary for alternate access of the transporter. BRD-9327 can be used for anti-tuberculosis study .
|
-
-
- HY-N6636
-
|
NF-κB
|
Inflammation/Immunology
|
Valencene is a sesquiterpene isolated from Cyperus rotundus, possesses antiallergic, antimelanogenesis, anti-infammatory, and antioxidant activitivies. Valencene inhibits the exaggerated expression of Th2 chemokines and proinflammatory chemokines through blockade of the NF-κB pathway. Valencene is used to flavor foods and drinks .
|
-
-
- HY-106305A
-
CI 958 trihydrochloride
|
DNA/RNA Synthesis
|
Cancer
|
Ledoxantrone (CI 958) trihydrochloride is a DNA helicases inhibitor with an IC50 of 0.17 μM. Ledoxantrone trihydrochloride can be used in the study of prostate cancer .
|
-
-
- HY-126635R
-
|
Adrenergic Receptor
Dopamine Receptor
|
Others
|
Mafoprazine (Standard) is the analytical standard of Mafoprazine. This product is intended for research and analytical applications. Mafoprazine is a phenylpiperazine derivative with variable affinities for neuronal receptors. It may exert its antipsychotic effects primarily through D2 receptor blockade and α-adrenergic activity, and may increase the activity of dopamine metabolites.
|
-
-
- HY-119385
-
|
Dopamine Receptor
|
Neurological Disease
|
Savoxepin mesylate is a D2 dopamine receptor (D2 Dopamine Receptor) antagonist with antipsychotic activity. Savoxepin mesylate selectively blocks dopamine D2 receptors in the hippocampus while having no significant effect on D2 receptors in the striatum. This selective blockade helps reduce the risk of extrapyramidal side effects (EPS) .
|
-
-
- HY-105925
-
MCN 2378
|
Adrenergic Receptor
|
Cardiovascular Disease
|
Mefenidil (MCN 2378) is a selective cerebral vasodilator that is not affected by beta-adrenergic blockade. Mefenidil can be used in the study of cardiovascular disease. In monkey models, mefenidil preferentially increases cerebral blood flow over systemic (femoral) blood flow. Mefenidil is also able to reduce systemic arterial pressure in anesthetized dogs.
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-
-
- HY-B0284A
-
|
Sodium Channel
|
Cardiovascular Disease
|
Nifedipine hydrochloride is a potent vasodilator with calcium antagonist activity. Nifedipine hydrochloride is a useful antianginal compound that can also lower blood pressure. Nifedipine hydrochloride exhibits comparable antihypertensive properties to some new compounds, especially in calcium channel blockade. Nifedipine hydrochloride is used in biological activity studies to develop new antihypertensive and/or antianginal compounds .
|
-
-
- HY-P4042
-
hepatitis B peptide 4980
|
HBV
|
Infection
Inflammation/Immunology
|
Hepatitis B Virus Receptor Binding Fragment (hepatitis B peptide 4980) is a synthetic peptide analog which specifically binds to Hep G2 cells. Hepatitis B Virus Receptor Binding Fragment is a promising immunogen expected to elicit protective antibodies based on the concept of the attachment blockade pathway of virus neutralization .
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-
-
- HY-131340
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
LASSBio-1632 is a new anti-asthmatic lead candidate associated with selective inhibition of PDE4A and PDE4D isoenzymes and blockade of airway hyper-reactivity (AHR) and TNF-α production in the lung tissue. LASSBio-1632 (7j) displays high experimental BBB permeability across BBB through passive diffusion .
|
-
-
- HY-122664
-
|
BRK
|
Cancer
|
XMU-MP-2 is a BRK inhibitor with significant inhibitory activity on BRK-positive cells. XMU-MP-2 inhibits oncogenic BRK-driven tumor growth in a mouse xenograft model. XMU-MP-2 also synergizes with HER2 inhibitors or endoplasmic reticulum (ER) blockade to exert antiproliferative activity .
|
-
-
- HY-129492
-
GNF4877
1 Publications Verification
|
DYRK
GSK-3
|
Metabolic Disease
|
GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells) .
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-
-
- HY-N6636R
-
|
NF-κB
|
Inflammation/Immunology
|
Valencene (Standard) is the analytical standard of Valencene. This product is intended for research and analytical applications. Valencene is a sesquiterpene isolated from Cyperus rotundus, possesses antiallergic, antimelanogenesis, anti-infammatory, and antioxidant activitivies. Valencene inhibits the exaggerated expression of Th2 chemokines and proinflammatory chemokines through blockade of the NF-κB pathway. Valencene is used to flavor foods and drinks .
|
-
-
- HY-P99406
-
MCLA 158
|
EGFR
|
Cancer
|
Petosemtamab (MCLA 158) is an anti- EGFR (Kd: 0.22 nM) and anti-LGR5 (Kd: 0.86 nM) monoclonal antibody (mAb). Petosemtamab leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab can be used in the research of solid tumors, such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC) .
|
-
-
- HY-117223
-
|
Potassium Channel
|
Neurological Disease
|
GEA 857 is a structural analog of the Serotonin (HY-B1473A) uptake blocker Alaproclate (HY-164011). GEA 857 enhances responses induced by muscarinic receptor agonists by inhibiting certain calcium-dependent potassium channels on membranes, a blockade that can enhance or prolong the muscarinic cholinergic effects. GEA 857 can be used in research on neurodegenerative diseases .
|
-
-
- HY-P9902A
-
MK-3475 (anti-PD-1); Lambrolizumab (anti-PD-1)
|
PD-1/PD-L1
|
Cancer
|
Pembrolizumab (anti-PD-1) is a humanized IgG4 antibody and PD-1 inhibitor. Pembrolizumab produces PD-1 blockade, preventing PD-L1 and PD-L2 from connecting to PD-1. This avoids the uncontrolled regulation of T cells on cells that normally express PD-1 .
|
-
-
- HY-W424918
-
|
Dopamine Receptor
|
Neurological Disease
|
Opromazine hydrochloride is an antipsychotic medication that exhibits sedative and antiemetic pharmacological effects, making it effective for treating psychiatric disorders such as schizophrenia and psychosis. Opromazine hydrochloride functions by reducing dopaminergic activity through the blockade of dopamine receptors in the brain. Opromazine hydrochloride has been analyzed for its metabolites in various microsomal enzymes, revealing differences in formation rates that underscore the variability of drug-metabolizing enzymes in human liver and placenta microsomes.
|
-
-
- HY-122140
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
ACG548B (compound 24) is a potent inhibitor of acetyl- and butyrylcholinesterase (AChE and BChE) with IC50s of 1.78 and 0.496 μM, respectively. ACG548B has higher AChE affinity and selectivity over BChE and ChoK (choline kinase) .
|
-
-
- HY-13954
-
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta .
|
-
-
- HY-121037
-
EGM1
|
Phosphodiesterase (PDE)
|
Cancer
|
Eggmanone (EGM1) is a potent and selective phosphodiesterase 4 (PDE4) antagonist with an IC50 of 72 nM for PDE4D3. Eggmanone shows approximately 40- to 50-fold selective for PDE4D3 over other PDEs. Eggmanone exerts its Hh-inhibitory effects through selective antagonism of PDE4, leading to protein kinase A activation and subsequent Hh blockade .
|
-
-
- HY-P5487
-
|
iGluR
|
Others
|
GluR23Y is a biological active peptide. (This GluR23Y peptide was used in ELISA cell-surface assay for the insulin-stimulated endocytosis of native AMPA receptors in cultured hippocampal neurons. GluR23Y prevented any insulin-induced reduction. The blockade of insulin action was observed when the GluR23Y peptide was delivered into neurons by fusing it to the membrane transduction domain of HIV-1.)
|
-
- HY-150587
-
|
ERK
NF-κB
|
Inflammation/Immunology
|
Anti-inflammatory agent 31 (enone 17) is a kind of andrographolide derivatives, is a anti-inflammatory agent. Anti-inflammatory agent 31 inhibits NF-κB activation by upstream blockade of PI3K/Akt and ERK1/2 MAPK activation. Anti-inflammatory agent 31 shows recovery effective of the intracellular GSH levels and protective effect on liver .
|
-
- HY-132246
-
|
MAGL
|
Neurological Disease
|
WWL123 analogue-1 is an analogue of WWL123. WWL123 is a potent and selective ABHD6 inhibitor with an IC50 of 430 nM . WWL123 crosses the blood-brain-barrier and inhibits ABHD6 in brain parenchyma. ABHD6 blockade by WWL123 exerts an antiepileptic effect in Pentylenetetrazole (PTZ)-induced epileptiform seizures and spontaneous seizures in R6/2 mice .
|
-
- HY-153543
-
|
Toll-like Receptor (TLR)
|
Cancer
|
TLR7/8 agonist 8 (compound 24m) is a potent toll-like receptor 7/8 (TLR7/8) dual agonist, with EC50s of 27 and 12 nM for hTLR7 and hTLR8, respectively. TLR7/8 agonist 8 can improve the antitumor activity of PD-1/PD-L1 blockade .
|
-
- HY-156677
-
|
METTL3
|
Cancer
|
STC-15 is an orally active RNA methyltransferase METTL3 inhibitor with the activity of activating anti-tumor immunity and reshaping the tumor microenvironment. STC-15 inhibits tumor growth by activating anti-cancer immune responses associated with increased interferon signaling and synergizes with T-cell checkpoint blockade. STC-15 can be used in the study of proliferative diseases such as cancer and autoimmune diseases .
|
-
- HY-13650
-
E 7070
|
Molecular Glues
Carbonic Anhydrase
|
Cancer
|
Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15 .
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-
- HY-103094
-
|
5-HT Receptor
|
Inflammation/Immunology
|
LY266097 hydrochloride is a selective 5-HT2B receptor antagonist with pKis of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2B receptor blockade contributes to the research in depression .
|
-
- HY-136310
-
|
PI5P4K
|
Cancer
|
PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC50s of 1.9 μM and 0.6 μM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways .
|
-
- HY-122171
-
|
Histamine Receptor
|
Neurological Disease
|
A-317920 is a selective and potent rat histamine H3 receptor (H3R) antagonist with pKi value of 9.2 and 7.0 for full-length rat and full-length human H3R, respectively. A-317920 exhibits over 130 fold selective affinity for the rat over the human H3R. A-317920 enhances cognition via H3R blockade .
|
-
- HY-161818
-
|
PD-1/PD-L1
|
Inflammation/Immunology
|
LLW-018 is a potent PD-1/PD-L1 inhibitor with an IC50 value of 2.61 nM. LLW-018 can interrupt PD-1/PD-L1 interaction with an IC50 value of 0.88 μM by cell-based PD-1/PD-L1 blockade bioassays. LLW-018 has the potential for immunotherapy research .
|
-
- HY-113695
-
|
Angiotensin-converting Enzyme (ACE)
Adrenergic Receptor
|
Cardiovascular Disease
|
BW A575C is a dual inhibitor against angiotensin converting enzyme (ACE) and β-adrenoceptor. BW A575C produces a competitive blockade of Isoprenaline (HY-108353)-induced tachycardia in a guinea-pig right atrial. BW A575C also inhibits Angiotensin I (HY-P1032)-induced pressor responses in rats. BW A575C is promising for research of hypertensive diseases .
|
-
- HY-16961
-
MGCD516; MG-516
|
VEGFR
c-Kit
FLT3
Discoidin Domain Receptor
Trk Receptor
|
Inflammation/Immunology
Cancer
|
Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
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-
- HY-155175
-
|
Tim3
|
Cancer
|
TIM-3-IN-2 (Compound A-41) is a Tim3 inhibitor (KD: 0.61 μM). TIM-3-IN-2 blocks TIM-3 interactions with PtdSer, CEACAM1, and Gal-9. TIM-3-IN-2 inhibits the immunosuppressive function of TIM-3. TIM-3-IN-2 reverses the TIM-3-mediated blockade of the production of proinflammatory cytokines, and maximizes the T-cell antitumor activity against AML cell lines .
|
-
- HY-16961A
-
MGCD516 malate; MG-516 malate
|
VEGFR
c-Kit
FLT3
Discoidin Domain Receptor
Trk Receptor
|
Inflammation/Immunology
Cancer
|
Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
|
-
- HY-128679
-
|
IKK
|
Cancer
|
TBK1/IKKε-IN-5 (compound 1) is an orally active TBK1 and IKKε dual inhibitor, with IC50 values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response to PD-1 and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used in cancer research, especially in tumour immunity .
|
-
- HY-P2265
-
|
Ras
|
Cancer
|
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
|
-
- HY-B0653
-
(S)-(-)-Bupivacaine
|
Sodium Channel
Ferroptosis
|
Neurological Disease
Cancer
|
Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
|
-
- HY-170525
-
|
CD73
|
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-153346
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RMC-6291
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Ras
ERK
Apoptosis
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Cancer
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Elironrasib is an orally active and covalent inhibitor of KRAS G12C(ON). Elironrasib forms a tri-complex within tumor cells between KRAS G12C(ON) and cyclophilin A (CypA). Thus, Elironrasib prevents KRAS G12C(ON) from signaling via steric blockade of RAS effector binding. Elironrasib inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. Elironrasib also inhibits the proliferation of KRAS G12C mutant cells with a median IC50 of 0.11 nM .
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- HY-B0653A
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(S)-(-)-Bupivacaine monohydrochloride
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Sodium Channel
Ferroptosis
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Cardiovascular Disease
Neurological Disease
Cancer
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Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
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- HY-P99406A
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EGFR
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Cancer
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Petosemtamab (FUT8-KO) is an anti-EGFR/LGR5 monoclonal antibody expressed by CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucose deficiency enhances the ADCC effect of the antibody. Petosemtamab (HY-P99406) is an anti-EGFR (Kd: 0.22 nM) and anti-LGR5 (Kd: 0.86 nM) monoclonal antibody (mAb). Petosemtamab leads to blockade of EGFR signaling and receptor degradation in LGR5+ cancer cells. Petosemtamab can be used in the study of solid tumors such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC), etc .
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- HY-B0653AS
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(S)-(–)-Bupivacaie-d9(hydrochloride)
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Isotope-Labeled Compounds
Ferroptosis
Sodium Channel
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Cardiovascular Disease
Neurological Disease
Cancer
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Levobupivacaine-d9 ((S)-(–)-Bupivacaie-d9) hydrochloride is deuterium labeled Levobupivacaine (hydrochloride). Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
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- HY-P2265A
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Ras
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Cancer
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SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
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- HY-132184
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5,6-EET; (±)5,6-EpETrE
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Adrenergic Receptor
Calcium Channel
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Endocrinology
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5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2.
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- HY-132184S
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5,6-EET-d11; (±)5,6-EpETrE-d11
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Isotope-Labeled Compounds
Adrenergic Receptor
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Endocrinology
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5,6-Epoxyeicosatrienoic acid-d11 (5,6-EET-d11) is deuterium labeled 5,6-Epoxyeicosatrienoic acid. 5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM. (±)5,6-Epoxyeicosatrienoic acid is provided as a mixture of the free acid and lactone .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P0142A
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PKG
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Cardiovascular Disease
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DT-3 acetate is a membrane-permeable protein kinase G Iα (PKG Iα) inhibitory peptide and shows pharmacological blockade of the cGMP-PKG signalling .
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- HY-P2265A
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Ras
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Cancer
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SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
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- HY-P0142
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PKG
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Cardiovascular Disease
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DT-3 is a membrane-permeable protein kinase G Iα (PKG Iα) inhibitory peptide and shows pharmacological blockade of the cGMP-PKG signalling .
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- HY-P4042
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hepatitis B peptide 4980
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HBV
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Infection
Inflammation/Immunology
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Hepatitis B Virus Receptor Binding Fragment (hepatitis B peptide 4980) is a synthetic peptide analog which specifically binds to Hep G2 cells. Hepatitis B Virus Receptor Binding Fragment is a promising immunogen expected to elicit protective antibodies based on the concept of the attachment blockade pathway of virus neutralization .
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- HY-P5487
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iGluR
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Others
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GluR23Y is a biological active peptide. (This GluR23Y peptide was used in ELISA cell-surface assay for the insulin-stimulated endocytosis of native AMPA receptors in cultured hippocampal neurons. GluR23Y prevented any insulin-induced reduction. The blockade of insulin action was observed when the GluR23Y peptide was delivered into neurons by fusing it to the membrane transduction domain of HIV-1.)
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- HY-P2265
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Ras
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Cancer
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SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99540
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PSB-205; QL1706 (iparomlimab/tuvonralimab); PBS105
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PD-1/PD-L1
CTLA-4
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Cancer
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Tuvonralimab (PSB-205; QL1706) is a dual immune checkpoint blockade containing a mixture of anti-PD-1 IgG4 and anti-CTLA-4 IgG1 antibodies, Iparomlimab and Tuvonralimab .
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- HY-P99406
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MCLA 158
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EGFR
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Cancer
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Petosemtamab (MCLA 158) is an anti- EGFR (Kd: 0.22 nM) and anti-LGR5 (Kd: 0.86 nM) monoclonal antibody (mAb). Petosemtamab leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab can be used in the research of solid tumors, such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC) .
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- HY-P9902A
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MK-3475 (anti-PD-1); Lambrolizumab (anti-PD-1)
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PD-1/PD-L1
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Cancer
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Pembrolizumab (anti-PD-1) is a humanized IgG4 antibody and PD-1 inhibitor. Pembrolizumab produces PD-1 blockade, preventing PD-L1 and PD-L2 from connecting to PD-1. This avoids the uncontrolled regulation of T cells on cells that normally express PD-1 .
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- HY-P99406A
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EGFR
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Cancer
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Petosemtamab (FUT8-KO) is an anti-EGFR/LGR5 monoclonal antibody expressed by CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucose deficiency enhances the ADCC effect of the antibody. Petosemtamab (HY-P99406) is an anti-EGFR (Kd: 0.22 nM) and anti-LGR5 (Kd: 0.86 nM) monoclonal antibody (mAb). Petosemtamab leads to blockade of EGFR signaling and receptor degradation in LGR5+ cancer cells. Petosemtamab can be used in the study of solid tumors such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC), etc .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0653AS
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Levobupivacaine-d9 ((S)-(–)-Bupivacaie-d9) hydrochloride is deuterium labeled Levobupivacaine (hydrochloride). Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
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- HY-132184S
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5,6-Epoxyeicosatrienoic acid-d11 (5,6-EET-d11) is deuterium labeled 5,6-Epoxyeicosatrienoic acid. 5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM. (±)5,6-Epoxyeicosatrienoic acid is provided as a mixture of the free acid and lactone .
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