货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V54240-1ml	10mM in DMSO	￥6760.00 V54240-1ml ￥6760.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V54240-1ml

10mM in DMSO

￥6760.00

货期：3-5天

产品描述：

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 K_i 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 K_i 较弱，分别为 481 nM 和 358 nM。

靶点：

BradykininReceptor

体外研究：

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[1].

体内研究：

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[1]. 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[2].

参考文献：

[1]. Gougat J, et al. SSR240612 [(2R)-2-[((3R)-3-(1,3-benzodioxol-5-yl)-3-[[(6-methoxy-2-naphthyl)sulfonyl]amino]propanoyl)amino]-3-(4-[[2R,6S)-2,6-dimethylpiperidinyl]methyl]phenyl)-N-isopropyl-N-methylpropanamide hydrochloride], a new nonpeptide antagonist o [Content Brief]

[2]. Dias JP, et al. The kinin B1 receptor antagonist SSR240612 reverses tactile and cold allodynia in an experimental rat model of insulin resistance. Br J Pharmacol. 2007 Sep;152(2):280-7. Epub 2007 Jul 9. [Content Brief]

溶解性：

DMSO : ≥ 100 mg/mL (126.04 mM)

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.26 ml	6.302 ml	12.604 ml
5 mM	0.252 ml	1.26 ml	2.521 ml
10 mM	0.126 ml	0.63 ml	1.26 ml
50 mM	0.025 ml	0.126 ml	0.252 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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