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Results for "

bradykinin antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Bradykinin Receptor (36) Akt (1) Amino Acid Derivatives (2) Angiotensin Receptor (2) Angiotensin-converting Enzyme (ACE) (1) Apoptosis (2) Biochemical Assay Reagents (1) Carboxypeptidase (1) Drug Intermediate (1) Endogenous Metabolite (1) ERK (2) Interleukin Related (1) mAChR (1) Neurotensin Receptor (1) PI3K (1) Prostaglandin Receptor (1) Reference Standards (2) TNF Receptor (1) Vasopressin Receptor (2)
By Research Areas:	Cancer (5) Cardiovascular Disease (8) Endocrinology (8) Inflammation/Immunology (16) Metabolic Disease (7) Neurological Disease (9)

By Targets:

Bradykinin Receptor (36)

Akt (1)

Amino Acid Derivatives (2)

Angiotensin Receptor (2)

Angiotensin-converting Enzyme (ACE) (1)

Apoptosis (2)

Biochemical Assay Reagents (1)

Carboxypeptidase (1)

Drug Intermediate (1)

Endogenous Metabolite (1)

ERK (2)

Interleukin Related (1)

mAChR (1)

Neurotensin Receptor (1)

PI3K (1)

Prostaglandin Receptor (1)

Reference Standards (2)

TNF Receptor (1)

Vasopressin Receptor (2)

By Research Areas:

Cancer (5)

Cardiovascular Disease (8)

Endocrinology (8)

Inflammation/Immunology (16)

Metabolic Disease (7)

Neurological Disease (9)

Inhibitors & Agonists

Peptides

Targets Recommended: Bradykinin Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-17446

Icatibant 10+ Cited Publications HOE 140	Bradykinin Receptor	Endocrinology
Icatibant (HOE-140) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC₅₀ and K_i of 1.07 nM and 0.798 nM respectively .

HY-108896

Icatibant acetate 10+ Cited Publications HOE 140 acetate	Bradykinin Receptor	Inflammation/Immunology
Icatibant acetate (HOE-140 acetate) is a potent and specific peptide antagonist of bradykinin B2 receptor with an IC₅₀ and K_i of 1.07 nM and 0.798 nM respectively .

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-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-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-W704574

Mergetpa	Carboxypeptidase Bradykinin Receptor Interleukin Related	Cardiovascular Disease Metabolic Disease
Mergetpa is a reversible Arg-carboxypeptidase inhibitor with high affinity. Mergetpa reduces B1R. Mergetpa blocks the overexpression of IL-1β protein and mRNA in glucose-fed rats. Mergetpa significantly increases the expression of IL-1β protein in the renal cortex. Mergetpa is used to block the conversion of kinins and B2 receptor antagonists into metabolites lacking the C-terminal arginine. Mergetpa inhibits the time-dependent enhancement of the response of isolated rabbit aorta to bradykinin. Mergetpa preserves the chemotactic activity of full-length SDF-1α on cells. Mergetpa reverses hyperglycemia, excessive weight gain, elevated levels of oxidative stress markers and overexpression of inflammatory markers in glucose-fed rats .

HY-168906

BI-113823	Bradykinin Receptor PI3K Akt TNF Receptor ERK	Neurological Disease Inflammation/Immunology
BI-113823 is an orally active, blood-brain barrier-permeable bradykinin B1 receptor antagonist, with a K_i value of 5.3 nM for human receptors and 13.3 nM for rat receptors. BI-113823 reduces inflammation-induced mechanical hyperalgesia, as well as the mechanical sensitivity of peripheral afferent nerves and spinal nociceptive-specific neurons. BI-113823 alleviates liver fibrosis and portal hypertension, and improves survival in chronic liver disease models. BI-113823 inhibits the activities of monocytes, neutrophils and hepatic stellate cells, as well as the PI3K/Akt signaling pathway. BI-113823 can be used in research related to inflammatory pain, liver fibrosis and portal hypertension .

HY-121156A

Anatibant hydrochloride LF 16-0687 hydrochloride; XY-2405 hydrochloride	Bradykinin Receptor	Neurological Disease
Anatibant (LF 16-0687; XY-2405) hydrochloride is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant hydrochloride binds to the human, rat and guinea-pig recombinant B2 receptor with K_i values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant hydrochloride crosses the blood-brain barrier (BBB). Anatibant hydrochloride can be used in research on brain damage diseases .

HY-P4676

Lys-(Des-Arg9,Leu8)-Bradykinin	Bradykinin Receptor	Inflammation/Immunology
Lys-(Des-Arg9,Leu8)-Bradykinin is a selective bradykinin B1 receptor (BDKRB1) antagonist. Lys-(Des-Arg9,Leu8)-Bradykinin inhibits local inflammatory edema. Lys-(Des-Arg9,Leu8)-Bradykinin induces the production of systemic acute-phase proteins. Lys-(Des-Arg9,Leu8)-Bradykinin is applicable to research related to peptidoglycan-polysaccharide-induced acute arthritis .

HY-147273

Fulimetibant	Bradykinin Receptor	Others
Fulimetibant is a Bradykinin receptor antagonist .

HY-W041989

Fmoc-Oic-OH	Amino Acid Derivatives Drug Intermediate Biochemical Assay Reagents	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-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-P1185

Antagonist G	Vasopressin Receptor Apoptosis	Cardiovascular Disease Cancer
Antagonist G is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy .

HY-P5518A

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

HY-15791

FR173657 FK-3657	Bradykinin Receptor	Inflammation/Immunology
FR173657 is an orally active bradykinin B2 receptor antagonist (IC₅₀: 0.56, 1.5, 2.9 nM for pig, rat, human B2 receptor respectively). FR173657 (p.o.) inhibits BK-induced bronchoconstriction in guinea-pigs (ED₅₀: 0.075 mg/kg). FR173657 (p.o.) also inhibits Carrageenin-induced paw oedema in mice (ED₅₀: 6.8 mg/kg). FR173657 can be used for research of inflammatory disease .

HY-121156

Anatibant LF 16-0687; XY-2405	Bradykinin Receptor	Neurological Disease
Anatibant (LF 16-0687; XY-2405) is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant binds to the human, rat and guinea-pig recombinant B2 receptor with K_i values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant crosses the blood-brain barrier (BBB). Anatibant can be used in research on brain damage diseases .

HY-P11405

[D-Arg1,D-Trp5,7,9,Leu11]-Substance P	Neurotensin Receptor	Neurological Disease Cancer
[D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P is a potent inhibitor of cell growth in small cell lung cancer (SCLC). [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P is also a neuropeptide antagonist, capable of blocking colony formation stimulated by various neuropeptides (including vasopressin and bradykinin). [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P inhibits the mobilization of Ca ²⁺ and the activation of mitogen-activated protein kinases induced by vasopressin or bradykinin. [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P inhibits the growth of H-69 xenograft tumors in nude 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-101368A

WIN 64338 hydrochloride	Bradykinin Receptor mAChR	Neurological Disease
WIN 64338 hydrochloride is a potent, selective, nonpeptide competitive antagonist of bradykinin B2 receptor. WIN 64338 hydrochloride inhibits [ ³H]-Bradykinin binding to the bradykinin B2 receptor on human IMR-90 cells with a K_i of 64 nM. WIN 64338 hydrochloride also can inhibits [ ³H]Quinuclidinyl benzilate binding to the rat brain muscarinic receptor (K_i=350 nM) .

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-106277A

Fasitibant chloride hydrochloride MEN16132	Bradykinin Receptor	Metabolic Disease
Fasitibant chloride hydrochloride (MEN16132) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B₂ (BK₂) receptor antagonist. Fasitibant chloride hydrochloride has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis .

HY-17446R

Icatibant (Standard) HOE 140 (Standard)	Reference Standards Bradykinin Receptor	Endocrinology
Icatibant (Standard) is the analytical standard of Icatibant. This product is intended for research and analytical applications. Icatibant (HOE-140) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC₅₀ and K_i of 1.07 nM and 0.798 nM respectively .

HY-108896R

Icatibant acetate (Standard) HOE 140 acetate (Standard)	Bradykinin Receptor Reference Standards	Inflammation/Immunology
Icatibant (acetate) (Standard) is the analytical standard of Icatibant (acetate). This product is intended for research and analytical applications. Icatibant acetate (HOE-140 acetate) is a potent and specific peptide antagonist of bradykinin B2 receptor with an IC50 and Ki of 1.07 nM and 0.798 nM respectively .

HY-10382

EXP-6803	Angiotensin Receptor	Cardiovascular Disease
EXP-6803 is a specific nonpeptide angiotensin II receptor antagonist with antihypertensive activity. EXP-6803 inhibits the contractile response to angiotensin II with a pA₂ value of 7.20. EXP-6803 effectively blocks responses to angiotensin I and II while not affecting responses to bradykinin or acetylcholine in guinea pig ileum. EXP-6803 can be used for hypertension research .

HY-123560

BKM-570	Bradykinin Receptor	Cancer
BKM-570 is a nonpeptide *bradykinin* antagonist with anticancer effects. BKM-570 can be used in the study of lung cancer, prostate cancer and ovarian cancer .

HY-19646

Zoliprofen 480156-S	Bradykinin Receptor Prostaglandin Receptor	Neurological Disease
Zoliprofen (480156-S), a new non-steroidal anti-inflammatory agent, has potent pain suppressing effect. Zoliprofen has strong antagonistic action against *bradykinin, markedly inhibiting all bradykinin*-induced edema and pain reactions. Zoliprofen weakly inhibits Arachidonic acid (HY-109590)-induced edema and pain reactions but also inhibits PGE2 synthesis of bovine vesicular gland microsomes .

HY-101368

WIN 64338	Bradykinin Receptor	Neurological Disease
WIN 64338 is a non-peptide bradykinin B2 receptor antagonist. WIN 64338 can inhibit bradykinin-evoked trigeminal nerve stimulation .

HY-P1185A

Antagonist G TFA	Vasopressin Receptor Apoptosis	Cancer
Antagonist G TFA is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy .

HY-15042A

(Rac)-MK 0686	Bradykinin Receptor	Metabolic Disease
(Rac)-MK 0686 is the racemate of MK 0686. MK 0686 is a bradykinin B₁ receptor antagonist .

HY-P3232

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

HY-P5518

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

HY-P2118

NPC-567	Bradykinin Receptor	Inflammation/Immunology
NPC-567 is a bradykinin B2 receptor antagonist. NPC-567 is effective in inhibiting the acute response to allergen in the airways .

HY-P1721

NPC 17731	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-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-106277

Fasitibant free base	Bradykinin Receptor	Metabolic Disease
Fasitibant (free base) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B₂ (BK₂) receptor antagonist. Fasitibant (free base) has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis .

HY-14886

Fasitibant chloride MEN16132 free base	Bradykinin Receptor	Cardiovascular Disease Neurological Disease
Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model .

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-103289

MEN 11270	Bradykinin Receptor	Metabolic Disease Inflammation/Immunology
MEN 11270, a cyclic decapeptide, is a *B2 kinin* receptor** antagonist. MEN 11270 bound with high-affinity to the B2 kinin receptor constitutively expressed by WI38 human fibroblasts, inhibiting 3H-bradykinin (BK) with a pK_i value of 10.3 .

HY-P1694

B4148	Bradykinin Receptor	Cardiovascular Disease
B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .

HY-121550

ME3221	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). ME3221's repeated administration in SHR results in sustained and stable hypotensive effects without affecting heart rate, indicating its potential for studying both renal and essential hypertension .

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-P4676A

Lys-(Des-Arg9,Leu8)-Bradykinin TFA	Bradykinin Receptor	Inflammation/Immunology
Lys-(Des-Arg9,Leu8)-Bradykinin TFA is a selective bradykinin B1 receptor (BDKRB1) antagonist. Lys-(Des-Arg9,Leu8)-Bradykinin TFA inhibits local inflammatory edema. Lys-(Des-Arg9,Leu8)-Bradykinin TFA induces the production of systemic acute-phase proteins. Lys-(Des-Arg9,Leu8)-Bradykinin TFA is applicable to research related to peptidoglycan-polysaccharide-induced acute arthritis .

HY-P1650

Breceptin B 9870	Bradykinin Receptor ERK	Cancer
Breceptin (B 9870) is an antagonist of the bradykinin B₁/B₂ receptor (B₁/B₂R). Breceptin exhibits an irreversible antagonist effect on B₂R, inhibiting the vasodilation induced by Bradykinin (HY-P0206) in the rabbit carotid vein contraction experiment. B-9870 shows partial agonist properties in HEK 293 cells with high expression of B₂R, and can activate ERK1/2 phosphorylation, calcium ion mobilization, arachidonic acid release, and receptor internalization. Breceptin can be used in research to inhibit breast cancer and non-small cell lung cancer .

HY-103294

R892	Endogenous Metabolite	Others
R892 is a selective and efficient bradyK_inin 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 .

HY-P0216A

A-779 TFA	Angiotensin Receptor	Cardiovascular Disease
A-779 TFA is a selective angiotensin-(1-7) (Ang-(1-7)) antagonist. A-779 TFA blocks Arachidonic acid release, bradykinin potentiation effects and hypotensive action. A-779 TFA exerts diuretic effects in non-pregnant rats, antidiuretic effects in late-pregnant rats, and also inhibits feed intake and water consumption in late-pregnant rats. A-779 TFA attenuates the regulatory effects of prostacyclin, nitric oxide and thromboxane A₂ associated with angiotensin-(1-7). A-779 TFA can be used in studies related to hypertension .

Cat. No.	Product Name	Target	Research Area