Bradykinin Receptor Antagonist

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

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.

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.

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.

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.

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

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.

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.

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.

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.

NPC-567 is a bradykinin B2 receptor antagonist. NPC-567 is effective in inhibiting the acute response to allergen in the airways.

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.

B 4310 is a non-organ-selective Bradykinin antagonist. B 4310 induces uterine contraction in rats. B 4310 blocks bradykinin-mediated responses, including substance P release, plasma extravasation, venous contraction, prostaglandin E₂ release and trigeminal nerve stimulation, but exerts no effect on angiotensin II, acetylcholine or capsaicin pathways. B 4310 exerts a reversible antagonistic effect on bradykinin-induced nociceptors. B 4310 serves as a tool for investigating the biological effects of bradykinin.

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.

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.