Bradykinin Receptor Antagonist

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.

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.

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.

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.

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

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.

Fulimetibant is a Bradykinin receptor antagonist.

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.

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.

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.

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.

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.

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.

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.

[Des-Arg10]-HOE I40 TFA is a potent bradykinin B1 receptor antagonist.

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).

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.

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.

B 9430 is a potent bradykinin B1/B2 receptor antagonist.

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.