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SB-649868 (GSK649868) 是一种有效的选择性口服活性食欲素拮抗剂,对 OX1 和 OX2 受体的 pKi 分别为 9.4 和 9.5。
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SB-649868 (GSK649868) 是一种有效的选择性口服活性食欲素拮抗剂,对 OX1 和 OX2 受体的 pKi 分别为 9.4 和 9.5。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 477 | 现货 | |
5 mg | ¥ 1,160 | 现货 | |
10 mg | ¥ 1,990 | 现货 | |
25 mg | ¥ 4,230 | 现货 | |
50 mg | ¥ 5,880 | 现货 | |
100 mg | ¥ 7,920 | 现货 | |
200 mg | ¥ 10,900 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,370 | 现货 |
产品描述 | SB-649868 (GSK649868) is a potent and selective orally active antagonist of orexin(pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively). |
靶点活性 | OX1:9.4 (pKi), OX2:9.5 (pKi) |
体外活性 | SB-649868 antagonizes orexin-A-induced inositol 1 phosphate (IP1) accumulation with the following pKB value (OX1=9.67;?OX2=9.64).?SB-649868 displaces the [3H]ACT-078573 receptor binding with the following pKi values: OX1=9.27;?OX2=8.91.?Increasing concentrations of SB-649868 (0.3 nM-30 nM) induces a rightward shift of the orexin-A CRCs with a depression of the agonist efficacy suggesting a clear non-surmountable behavior.?The calculated apparent pKb values are 9.67 0.03 and 9.64 0.07 for OX1 and OX2 |
别名 | GSK649868 |
分子量 | 477.55 |
分子式 | C26H24FN3O3S |
CAS No. | 380899-24-1 |
Smiles | Cc1nc(C(=O)N2CCCC[C@H]2CNC(=O)c2cccc3occc23)c(s1)-c1ccc(F)cc1 |
密度 | 1.305 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 100 mg/mL (209.40 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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