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CAS No. : 464930-42-5
MCE 国际站:SSR240612
产品活性:SSR240612 是一种有效的,可口服的,特异性的非肽类缓激肽 B1 (bradykinin B1) 受体拮抗剂,对 bradykinin B1 受体(在人 MRC5 细胞和表达人 B1 受体的 HEK 细胞)的 Ki 值分别为 0.48 nM,0.73 nM;对 B2 受体 (在豚鼠回肠膜和表达人 B1 受体的 CHO 细胞) 的 Ki 较弱,分别为 481 nM 和 358 nM。
研究领域:GPCR/G Protein
作用靶点:Bradykinin Receptor
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.
相关产品:Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Immunology/Inflammation Compound Library | Endocrinology Compound Library | Orally Active Compound Library | Neurotransmitter Receptor Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | Lobradimil | Bradykinin (1-7) | Fasitibant free base | Lys-[Hyp3]-Bradykinin | WIN 64338 hydrochloride | FR167344 free base | Icatibant | Lys-[Des-Arg9]Bradykinin TFA | ELN-441958 | Bombinakinin M | [Tyr8] Bradykinin | Fulimetibant | [Hyp3]-Bradykinin | [Des-Arg9]-Bradykinin acetate | Bradykinin (1-6) | Bradykinin (2-9) | Bradykinin | Bradykinin (1-5) | B 9430 | MEN 11270 | Retrobradykinin | Methionyl-Lysyl-Bradykinin | Lys-[Des-Arg9]Bradykinin | Lys-Bradykinin | Deucrictibant
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