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Results for "

B1 antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (6) Amino Acid Derivatives (2) Amyloid-β (2) Apoptosis (1) Aryl Hydrocarbon Receptor (1) Autophagy (1) Bradykinin Receptor (12) Calcium Channel (1) CCR (1) Cholinesterase (ChE) (2) Complement System (1) Cytochrome P450 (2) Dopamine Receptor (1) GABA Receptor (1) HCV (1) iGluR (7) MDM-2/p53 (1) mGluR (1) p38 MAPK (1) Potassium Channel (2) RSV (1) Sigma Receptor (1)
By Research Areas:	Cancer (2) Cardiovascular Disease (1) Endocrinology (5) Infection (2) Inflammation/Immunology (10) Metabolic Disease (2) Neurological Disease (14)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-19900

ITX5061 2 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).

HY-15039

SSR240612	Bradykinin Receptor	Metabolic Disease Inflammation/Immunology Endocrinology
SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with K_is 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.

HY-15043

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

HY-P4676

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

HY-103290

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

HY-158262

*Bradykinin B1 receptor antagonist* 1**	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 .

HY-P2109

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

HY-P3232

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

HY-W041989

Fmoc-Oic-OH	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 .

HY-W013153

Fmoc-D-Tic-OH	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 .

HY-100301

FR167344 free base	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.

HY-10799

EG00229 trifluoroacetate Maximum Cited Publications 8 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 .

HY-100827

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

HY-15041

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

HY-15042

MK 0686	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 .

HY-101343

RS 39604	5-HT Receptor	Neurological Disease
RS 39604 is a potent, selective, and orally active 5-HT₄ receptor antagonist with a pK_i of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pK_i<6.5) for 5-HT_1A, 5-HT_2C, 5-HT₃, α_1c, D₁, D₂, M₁, M₂, AT₁, B₁ and opioid mu receptors and moderate affinity for δ₁, (pK_i=6.8) and δ₂ (pK_i=7.8) sites .

HY-155061

hCYP1B1-IN-1	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 .*

HY-101356

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

HY-114097A

*CCR1 antagonist* 11 hydrochloride**	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 .

HY-126123

*NR2B-selective NMDA receptor antagonist* 1**	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 .

HY-14348

GSK163090	5-HT Receptor Dopamine Receptor	Neurological Disease
GSK163090 is a potent, selective and orally active 5-HT_1A/1B/1D receptor antagonist with pK_i values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pK_i value of 6.1. GSK163090 has antidepressant and anxiolytic activities .

HY-P3209

Des-Arg9-[Leu8]-Bradykinin acetate	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 .

HY-121392

GR 125743	5-HT Receptor	Cardiovascular Disease Neurological Disease
GR 125743 is a selective *5-HT_1B/1D* receptor antagonist, with pK_is of 8.85 and 8.31 for wild-type h5-HT_1B and wild-type h5-HT_1D, respectively. GR 125743 is used for the research of Parkinson's disease and cardiovascular diseases .

HY-101043

4-PPBP maleate	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 .

HY-107707

TCS 46b	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.

HY-100794

GR127935 hydrochloride	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 .

HY-N6771

Cyclopiazonic acid 3 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].

HY-107018

AR-A 2 AR-A 000002	5-HT Receptor	Neurological Disease
AR-A 2 is a selective 5-HT_1B receptor antagonist, with high affinity to guinea pig cortex *5HT_1B/1D* and recombinant guinea pig 5-HT_1B receptors (K_i=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT_1D receptor (K_i, 5 nM), and shows an EC₅₀ of 4.5 nM for the guinea pig 5-HT_1B receptor; AR-A 2 can be used in the research of depression and anxiety.

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) .

HY-155733

AChE/Aβ-IN-1	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 .

HY-155735

AChE/Aβ-IN-2	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 .

HY-12882A

Ifenprodil tartrate 4 Publications Verification	iGluR Potassium Channel	Neurological Disease
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 .

HY-B0822S1

Fipronil-13C6	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.

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

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

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

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

[Des-Arg10]-HOE I40	Peptides	Others
[Des-Arg10]-HOE I40 is a biological active peptide. (A potent B1 bradykinin receptor antagonist.)

Fmoc-Oic-OH	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-D-Tic-OH	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 .

Des-Arg9-[Leu8]-Bradykinin acetate	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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N6771

Cyclopiazonic acid 3 Publications Verification	Alkaloids Structural Classification Microorganisms Pyrrole Alkaloids Classification of Application Fields Source classification Other Diseases Disease Research Fields Indole Alkaloids	Calcium Channel 5-HT Receptor MDM-2/p53 Apoptosis RSV
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].

HY-12882A

Ifenprodil tartrate 4 Publications Verification	Alkaloids Piperidine Alkaloids Neurological Disease Classification of Application Fields Crassulaceae Source classification Sedum sarmentosum Bunge Plants Disease Research Fields	iGluR Potassium Channel
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 .

Cat. No.	Product Name	Chemical Structure

HY-B0822S1

Fipronil-13C6

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.

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