SSR240612
规格
| Cas Number | 464930-42-5 |
| 规格或纯度 | ≥95% |
| 纯度 | ≥95% |
| 包装 | 10mg 或 1mg 或 5mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | DMSO : ≥ 100 mg/mL (126.04 mM) |
| 过滤标签 | Bradykinin Receptor,GPCR/G Protein |
| 储存温度 | 2-8°C储存,干燥 |
| 运输条件 | 冰袋运输 |
| 物理形态 | 固体 |
| 生化和生理学机理 | SSR240612 是一种强效的口服活性特异性非肽缓激肽 B1 受体拮抗剂，对表达人 B1 受体的人成纤维细胞 MRC5 和 HEK 细胞的 B1 激肽受体的 K i s 分别为 0.48 nM 和 0.73 nM，对 B2 受体的 K i s 分别为 481 nM 和 358 nM。 |
| 英文描述 |
SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with K i s 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. In Vitro SSR240612 is a potent bradykinin B1 receptor antagonist, with K i s 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 IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 ID 50 s 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:Ki: 0.48 nM (bradykinin B1 receptor, Human MRC5), 0.73 nM (bradykinin B1 receptor, Human HEK-B1), 481 nM (bradykinin B2 receptor, guinea pig ileum membranes), 358 nM (bradykinin B2 receptor, Human CHO-B2) |