SSR240612

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SSR240612 是一种有效的口服活性特异性非肽缓激肽 B1 受体拮抗剂（B1 和 B2 受体的 Kis 分别为 0.48-0.73 和 358-481 nM）。

SSR240612 is a potent and orally active specific non-peptide bradykinin B1 receptor antagonist (Kis = 0.48-0.73 and 358-481 nM for B1 and B2 receptors respectively).(In Vitro):SSR240612 is a potent bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B2 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B1 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively. SSR240612 inhibits inositol phosphate 1 formation with an IC50 of 1.9 nM, but shows no obvious effect on inositol phosphate-1 formation induced by BK (3 nM) activation of B2 receptor in human fibroblast MRC5.(In Vivo):SSR240612 (10 mg/kg p.o. or 0.3, 1 mg/kg i.p.) obviously blocks the des-Arg9-BK-induced paw edema in the mice. SSR240612 (10 and 30 mg/kg) reduces the duration of the late phase of paw licking in a dose dependent manner in the formalin model of inflammation in mice. SSR240612 (0.3, 3, and 30 mg/kg, p.o.) treatment before capsaicin potently and non-concentration-dependently reduces the ear edema. SSR240612 (0.3 mg/kg, i.v.) also suppresses the tissue destruction and neutrophil accumulation in the rat intestine, after splanchnic artery occlusion/reperfusion. Moreover, SSR240612 (1 and 3 mg/kg p.o.) dramacally increases the withdrawal latencies in the thermal hyperalgesia induced by UV irradiation in rats. SSR240612 inhibits tactile and cold allodynia at 3?h in glucose-fed rats but had no effect in control rats with ID50s of 5.5 and 7.1?mg/kg, respectively. SSR240612 shows no effect on plasma glucose and insulin, insulin resistance (HOMA index) and aortic superoxide anion production in glucose-fed rats at 10?mg/kg.

SSR240612 is a potent bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B2 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B1 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively. SSR240612 inhibits inositol phosphate 1 formationwith an IC50 of 1.9 nM, but shows no obvious effect on inositol phosphate-1 formation induced by BK (3 nM) activation of B2 receptor in human fibroblast MRC5.

SSR240612 (10 mg/kg p.o. or 0.3, 1 mg/kg i.p.) obviously blocks the des-Arg9-BK-induced paw edema in the mice. SSR240612 (10 and 30 mg/kg) reduces the duration of the late phase of paw licking in a dose dependent manner in the formalin model of inflammation in mice. SSR240612 (0.3, 3, and 30 mg/kg, p.o.) treatment before capsaicin potently and non-concentration-dependently reduces the ear edema. SSR240612 (0.3 mg/kg, i.v.) also suppresses the tissue destruction and neutrophil accumulation in the rat intestine, after splanchnic artery occlusion/reperfusion. Moreover, SSR240612 (1 and 3 mg/kg p.o.) dramacally increases the withdrawal latencies in the thermal hyperalgesia induced by UV irradiation in rats. SSR240612 inhibits tactile and cold allodynia at 3?h in glucose-fed rats but had no effect in control rats with ID50s of 5.5 and 7.1?mg/kg, respectively. SSR240612 shows no effect on plasma glucose and insulin, insulin resistance (HOMA index) and aortic superoxide anion production in glucose-fed rats at 10?mg/kg.

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GPCR/G Protein

Bradykinin Receptor

B1 Receptor

Neurological Disease

CNS disorders; Inflammation; Neuropathic pain; Pain

464930-42-5

793.41

C42H53ClN4O7S

>98% (HPLC)

DMSO: 100 mg/mL (126 mM);Water: Insoluble

Cl.COc1ccc2cc(ccc2c1)S(=O)(=O)N[C@H](CC(=O)N[C@H](Cc1ccc(CN2[C@@H](C)CCC[C@H]2C)cc1)C(=O)N(C)C(C)C)c1ccc2OCOc2c1

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(-20℃)

With Ice Pack

≥ 2 years