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B1 antagonist

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49

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10

Peptides

3

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1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-19900
    ITX5061
    3 Publications Verification

    p38 MAPK Autophagy HCV Infection
    ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1).
    ITX5061
  • HY-15039

    Bradykinin Receptor Metabolic Disease Inflammation/Immunology Endocrinology
    SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.
    SSR240612
  • HY-15043

    Bradykinin Receptor Inflammation/Immunology Endocrinology
    ELN-441958 is a potent, neutral, competitive and selective bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse .
    ELN-441958
  • HY-P5518A

    Bradykinin Receptor Inflammation/Immunology Endocrinology
    [Des-Arg10]-HOE I40 TFA is a potent bradykinin B1 receptor antagonist .
    [Des-Arg10]-HOE I40 TFA
  • HY-P4676

    Bradykinin Receptor Endocrinology
    Lys-(Des-Arg9,Leu8)-Bradykinin is a bradykinin B1 receptor antagonist .
    Lys-(Des-Arg9,Leu8)-Bradykinin
  • HY-158262

    Bradykinin Receptor Neurological Disease
    Bradykinin B1 receptor antagonist 1 (compound 6B) is a potent and cross the blood-brain barrier bradykinin B1 antagonist. Bradykinin B1 receptor antagonist 1 has the potential for the research of pain .
    Bradykinin B1 receptor antagonist 1
  • HY-P2109

    Bradykinin Receptor Inflammation/Immunology
    JMV-1645 is a potent and selective B1 bradykinin receptor antagonist with a Ki value of 0.023 nM on the human cloned B1 receptor. JMV-1645 can be utilized in trauma and infection research .
    JMV-1645
  • HY-P3232

    Bradykinin Receptor Inflammation/Immunology Endocrinology
    B 9430 is a potent bradykinin B1/B2 receptor antagonist .
    B 9430
  • HY-103294

    Endogenous Metabolite Others
    R892 is a selective and efficient bradyKinin B1 receptor antagonist with significant antagonistic activity. The pA2 values of R892 in human and rabbit B1 receptors are 8.8 and 8.6 respectively, indicating its strong anti-activity at these receptors. R892 exhibits selectivity with ID50 values of 2.8 nM and >600 nM for B1 and B2 receptors, respectively, and has no endogenous agonist activity. R892 is resistant to aminopeptidase and kininase II (ACE) degradation and exhibits metabolic stability .
    R892
  • HY-P5518

    Bradykinin Receptor Inflammation/Immunology Endocrinology
    [Des-Arg10]-HOE I40 is a potent bradykinin B1 receptor antagonist .
    [Des-Arg10]-HOE I40
  • HY-103290

    Bradykinin Receptor Others
    R715 is a selective bradykinin B1 receptor antagonist. R715 significantly attenuates the hyperalgesic effect developed in Streptozotocin(HY-13753)-diabetic mice .
    R715
  • HY-W041989

    Amino Acid Derivatives Others
    Fmoc-Oic-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize bioactive peptide mimetics, such as [desArg 10]HOE 140, which has bradykinin B1 antagonist activity .
    Fmoc-Oic-OH
  • HY-W013153

    Amino Acid Derivatives Others
    Fmoc-D-Tic-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize bioactive peptide mimetics, such as [desArg 10]HOE 140, which has bradykinin B1 antagonist activity .
    Fmoc-D-Tic-OH
  • HY-100301

    Bradykinin Receptor Inflammation/Immunology Endocrinology
    FR167344 free base is an orally active, nonpeptide bradykinin receptor B2 antagonist. FR167344 free base shows a high affinity binding to the B2 receptor with an IC50 value of 65 nM and no binding affinity for the B1 receptor.
    FR167344 free base
  • HY-10799
    EG00229 trifluoroacetate
    Maximum Cited Publications
    7 Publications Verification

    Complement System Cancer
    EG00229 is a neuropilin 1 (NRP1) receptor antagonist. EG00229 selectively inhibits VEGF-A binding to NRP1 b1 domain with an IC50 of 3 μM, but has no effect on VEGFA binding to VEGFR-1 and VEGFR-2 .
    EG00229 trifluoroacetate
  • HY-100827

    LF22-0542

    Bradykinin Receptor Inflammation/Immunology
    Safotibant (LF22-0542) is a selective antagonist for kinin B1 receptor (BKB1R), with Ki of 0.35 and 6.5 nM, for human and mouse BKB1R, respectively. Safotibant exhibits analgesic and anti-inflammatory property in mice model .
    Safotibant
  • HY-168906

    Bradykinin Receptor Neurological Disease Inflammation/Immunology
    BI-113823 is an orally active and selective bradykinin B1 receptor antagonist. BI-113823 can reduce complete Freund's adjuvant (HY-153808)-induced mechanical hyperalgesia in rats. BI-113823 can be used for the research of chronic inflammatory pain .
    BI-113823
  • HY-15041

    Bradykinin Receptor Inflammation/Immunology
    NVP-SAA164 is an orally active nonpeptide kinin B1 receptor antagonist. NVP-SAA164 reverses CFA (Complete Freund's adjuvant) (HY-153808)-induced mechanical hyperalgesia and desArg10KD-induced hyperalgesia in hB1-KI mice, and is inactive in a model of inflammatory pain in wild-type mice .
    NVP-SAA164
  • HY-17617

    Z-360

    Cholecystokinin Receptor Ephrin Receptor Interleukin Related VEGFR HIF/HIF Prolyl-Hydroxylase Akt Neurological Disease Cancer
    Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [ 3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain .
    Nastorazepide
  • HY-101343

    5-HT Receptor Neurological Disease
    RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites .
    RS 39604
  • HY-15042

    Bradykinin Receptor Metabolic Disease
    MK 0686, a potent bradykinin B1 receptor antagonist, demonstrates autoinduction of metabolism in rhesus monkeys after oral administration. It undergoes significant biotransformation primarily via oxidation pathways, leading to the formation of metabolites like M11 and M13 in rhesus liver microsomes. This metabolic induction is mediated by CYP2C75, as evidenced by increased mRNA expression, protein levels, and catalytic activity of this enzyme in hepatocytes and liver microsomes from MK 0686-treated animals. The autoinduction phenomenon suggests that MK 0686 enhances its own metabolism by upregulating CYP2C75, potentially influencing its systemic exposure and pharmacokinetics over time .
    MK 0686
  • HY-14575

    Z-360 hemicalcium

    Cholecystokinin Receptor Ephrin Receptor Interleukin Related VEGFR HIF/HIF Prolyl-Hydroxylase Akt Neurological Disease Cancer
    Nastorazepide (Z-360) hemicalcium is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide hemicalcium inhibits the specific binding of [ 3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide hemicalcium inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide hemicalcium has antitumor activity against pancreatic cancer. Nastorazepide hemicalcium inhibits colorectal cancer liver metastasis and relieves pain .
    Nastorazepide hemicalcium
  • HY-17617R

    Cholecystokinin Receptor Ephrin Receptor Interleukin Related VEGFR HIF/HIF Prolyl-Hydroxylase Akt Neurological Disease Cancer
    Nastorazepide (Standard) is the analytical standard of Nastorazepide. This product is intended for research and analytical applications. Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain .
    Nastorazepide (Standard)
  • HY-W008038

    iGluR Others
    NMDAR antagonist 3 (Compound 2) is an antagonist of the NMDA receptor. NMDAR antagonist 3 has a certain but weak inhibitory activity against the NR1A/2B subtype of the NMDA receptor .
    NMDAR antagonist 3
  • HY-155061

    Cytochrome P450 Aryl Hydrocarbon Receptor Cancer
    hCYP1B1-IN-1 (compound B18) is a hCYP1B1 inhibitor (IC50=3.6 nM),as well as an antagonist of Aryl Hydrocarbon Receptor. hCYP1B1-IN-1 exhibtis suitable metabolic stability and good cell-permeability. hCYP1B1-IN-1 inhibits migration of MCF-7 cells .
    hCYP1B1-IN-1
  • HY-101356

    mGluR Neurological Disease
    CPCCOEt is a low affinity, selective, non-competitive and reversible antagonist of metabotropic glutamate receptor 1b (mGluR1b) .
    CPCCOEt
  • HY-114097A

    CCR Inflammation/Immunology
    CCR1 antagonist 11 hydrochloride (A1B1) is an orally active CCR1 antagonist with the IC50 values of 0.03 μM, 0.58 μM and 0.32 μM for hCCR1, mCCR1 and rCCR1, respectively. CCR1 antagonist 11 hydrochloride can be used in the study of rheumatoid arthritis and other related inflammatory diseases .
    CCR1 antagonist 11 hydrochloride
  • HY-126123

    iGluR Potassium Channel Neurological Disease
    NR2B-selective NMDA receptor antagonist 1 (compound 29) is a potent antagonist of NR1/NR2B receptors, with IC50s of 0.05 μM, 0.73 μM, 2.4 μM to NR1/NR2B NMDA receptor, hERG, α1-AdR, respectivity. NR2B-selective NMDA receptor antagonist 1 exhibites efficient permeability across the blood–brain barrier .
    NR2B-selective NMDA receptor antagonist 1
  • HY-114246

    Androgen Receptor Cancer
    ONC1-13B is a potent androgen receptor (AR) antagonist with the activity of effectively inhibiting PSA expression in prostate cancer cells. ONC1-13B can effectively inhibit PSA expression and prostate cancer cell proliferation under DHT stimulation. ONC1-13B exerts its anti-tumor effect by preventing androgen from binding to AR and its nuclear translocation .
    ONC1-13B
  • HY-14348

    5-HT Receptor Dopamine Receptor Neurological Disease
    GSK163090 is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK163090 has antidepressant and anxiolytic activities .
    GSK163090
  • HY-P3209

    Bradykinin Receptor Inflammation/Immunology
    Des-Arg9-[Leu8]-Bradykinin acetate is potent bradykinin receptor 1 (B1R) antagonist. Des-Arg9-[Leu8]-Bradykinin acetate can be used for renal fibrosis research .
    Des-Arg9-[Leu8]-Bradykinin acetate
  • HY-121392

    5-HT Receptor Cardiovascular Disease Neurological Disease
    GR 125743 is a selective 5-HT1B/1D receptor antagonist, with pKis of 8.85 and 8.31 for wild-type h5-HT1B and wild-type h5-HT1D, respectively. GR 125743 is used for the research of Parkinson's disease and cardiovascular diseases .
    GR 125743
  • HY-169187

    Bacterial Cancer
    Antibacterial agent 247 (compund 30b) is a bacterial antagonist that significantly inhibits the formation of Pseudomonas aeruginosa biofilm (IC50=5.8 μM) and multiple virulence phenotypes, and enhances its interaction with Tob Antibacterial activity of combined therapy with ampicillin and polymyxin B .
    Antibacterial agent 247
  • HY-101043

    Sigma Receptor iGluR Neurological Disease
    4-PPBP maleate is a potent σ 1 receptor ligand and agonist. 4-PPBP maleate is a non-competitive, selective NR1a/2B NMDA receptors (expressed in Xenopus oocytes) antagonist. 4-PPBP maleate provides neuroprotection .
    4-PPBP maleate
  • HY-107707

    iGluR Neurological Disease
    TCS 46b (Compound 46b) is a potent, selective and orally active NMDA NR1A/2B receptor antagonist with an IC50 of 5.3 nM . TCS 46b is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    TCS 46b
  • HY-100794

    5-HT Receptor Neurological Disease
    GR127935 hydrochloride is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. GR127935 hydrochloride has 100-fold selectivity for 5-HT1B/1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 hydrochloride can be used in neurological disease research .
    GR127935 hydrochloride
  • HY-123869

    5-HT Receptor Neurological Disease
    GR127935 is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. GR127935 hydrochloride has 100-fold selectivity for 5-HT1B/1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 can be used in neurological disease research .
    GR127935
  • HY-N6771
    Cyclopiazonic acid
    4 Publications Verification

    Calcium Channel 5-HT Receptor MDM-2/p53 Apoptosis RSV Infection
    Cyclopiazonic acid is an endoplasmic reticulum calcium ATPase (ECAs) inhibitor and human respiratory syncytial virus (RSV) inhibitor (EC50 value of 4.13 μ M), which can reduce the antagonistic effect of 5-HT receptors in rat thoracic aorta, induce p53 dependent cell apoptosis and reproductive toxicity in mouse testes, and inhibit the biological activation of aflatoxin B [1][4][5].
    Cyclopiazonic acid
  • HY-172884

    Cholinesterase (ChE) iGluR Neurological Disease
    MDAR IN-1 (Compound 5m) is a brain-penetrant inhibitor of acetylcholinesterase (AChE) and antagonist of the GluN1/GluN2B subtype of NMDAR receptor. MDAR IN-1 effectively inhibits AChE activity, enhances cholinergic neurotransmission, and blocks NMDAR, reducing excitatory neurotoxicity. MDAR IN-1 is promising for research of Alzheimer's disease .
    MDAR-IN-1
  • HY-13457
    TCN 201
    1 Publications Verification

    iGluR Neurological Disease
    TCN 201 is a potent, selective and non-competitive antagonist of GluN1/GluN2A NMDA receptor, with a pIC50 of 6.8. TCN 201 is selective for GluN1/GluN2A NMDA receptor over GluN1/GluN2B NMDA receptor (pIC50<4.3) .
    TCN 201
  • HY-107018

    AR-A 000002

    5-HT Receptor Neurological Disease
    AR-A 2 is a selective 5-HT1B receptor antagonist, with high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki, 5 nM), and shows an EC50 of 4.5 nM for the guinea pig 5-HT1B receptor; AR-A 2 can be used in the research of depression and anxiety.
    AR-A 2
  • HY-155735

    iGluR Cholinesterase (ChE) Amyloid-β Neurological Disease
    AChE/Aβ-IN-2 (compound 33) is a potent and orally active inhibitor of acetylcholinesterase (AChE) with IC50 of 135 nM, as well as an antagonist of NMDA receptor (GluN1-1b/GluN2B subunit combination) with IC50 of 5.054 μM. AChE/Aβ-IN-2 also inhibits Aβ aggregation and shows good blood-brain barrier permeability. AChE/Aβ-IN-2 improves cognitive and spatial memory impairment in rats model .
    AChE/Aβ-IN-2
  • HY-155733

    iGluR Cholinesterase (ChE) Amyloid-β Neurological Disease
    AChE/Aβ-IN-1 (compound 32) is a potent and orally active inhibitor of acetylcholinesterase (AChE) with an IC50 of 86 nM, as well as an antagonist of NMDA receptor (GluN1-1b/GluN2B subunit combination) with IC50 of 3.876 μM. AChE/Aβ-IN-1 also inhibits Aβ aggregation and shows good blood-brain barrier permeability and neuroprotection. AChE/Aβ-IN-1 improves cognitive and spatial memory impairment in rats model .
    AChE/Aβ-IN-1
  • HY-12882
    Ifenprodil
    Maximum Cited Publications
    7 Publications Verification

    NP-120; RC-61-91

    iGluR Adrenergic Receptor Potassium Channel Calcium Channel Influenza Virus Infection Neurological Disease
    Ifenprodil (NP-120), a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil is an α1 adrenergic receptor antagonist. Ifenprodil inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease .
    Ifenprodil
  • HY-172213

    iGluR Neurological Disease
    (3S,6R)-NML is a NMDA receptor antagonist, with pIC50s of 4.8 (GluN1-GluN2A), 4.6 (GluN1-GluN2B), 5.0 (GluN1-GluN2C), 5.0 (GluN1-GluN2D) respectively. (3S,6R)-NML can be used for depression research .
    (3S,6R)-NML
  • HY-12882A
    Ifenprodil tartrate
    Maximum Cited Publications
    7 Publications Verification

    NP-120 tartrate; RC-61-91 tartrate

    iGluR Adrenergic Receptor Potassium Channel Calcium Channel Influenza Virus Infection Neurological Disease
    Ifenprodil (NP-120) tartrate, a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate is an α1 adrenergic receptor antagonist. Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil tartrate has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil tartrate can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease .
    Ifenprodil tartrate
  • HY-B0822S1

    GABA Receptor Cytochrome P450 Inflammation/Immunology
    Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
    Fipronil-13C6
  • HY-12882AR

    NP-120 tartrate (Standard); RC-61-91 tartrate (Standard)

    iGluR Potassium Channel Neurological Disease
    Ifenprodil (tartrate) (Standard) is the analytical standard of Ifenprodil (tartrate). This product is intended for research and analytical applications. Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator .
    Ifenprodil tartrate (Standard)
  • HY-12962A

    iGluR Neurological Disease
    NMDA-IN-1 dihydrochloride is a selective NMDA NR2B antagonist with a Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM. NMDA-IN-1 dihydrochloride inhibits Glu/Gly stimulated Ca2+ flux in Ltk- cells expressing the hNR1a/NR2B with a IC50 of 9.7 nM. NMDA-IN-1 dihydrochloride has no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor. NMDA-IN-1 dihydrochloride shows excellent activity in the mechanical hyperalgesia assay in rats. NMDA-IN-1 dihydrochloride can be used for the study of stroke, Parkinson, and neuropathic pain .
    NMDA-IN-1 dihydrochloride

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