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Bradykinin B2 Receptor Antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Bradykinin Receptor (19) Carboxypeptidase (1) Endogenous Metabolite (1) ERK (1) Interleukin Related (1) mAChR (1) Reference Standards (2)
By Research Areas:	Cancer (1) Cardiovascular Disease (2) Endocrinology (5) Inflammation/Immunology (8) Metabolic Disease (5) Neurological Disease (5)

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-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-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-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-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-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-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-P3232

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

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-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-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-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-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-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 .

Cat. No.	Product Name	Target	Research Area

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-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-P3232

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

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-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-P5493

D-Arg-[Hyp3,Thi5,8,D-Phe7]-Bradykinin	Peptides	Others
D-Arg-[Hyp3,Thi5,8,D-Phe7]-Bradykinin is a biological active peptide. (inhibited bradykinin-induced contractions concentration dependently; bradykinin B2 receptor antagonist)

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 .

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