生物活性
Cobicistat (GS-9350)是有效，选择性的细胞色素酶P450 3A (CYP3A)抑制剂，包括重要的cyp3a4亚型。它还抑制肠道转运蛋白，增加几种hiv药物的整体吸收，包括atazanavir、darunavir和tenofovir alafenamide延胡索酸盐。
靶点信息
化学数据
| 目录号 | A11277 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 766.0 |
| Formula | C40H53N7O5S2 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 1004316-88-4 |
| Synonyms | GS9350 |
| SMILES | CC(C)C1=NC(=CS1)CN(C)C(=O)N[C@@H](CCN2CCOCC2)C(=O)N[C@H](CC[C@H](CC3=CC=CC=C3)NC(=O)OCC4=CN=CS4)CC5=CC=CC=C5 |
溶解度
| In vitro (25°C) | DMSO | 85 mg/mL (109.53 mM) |
| Water | Insoluble |
| Ethanol | 85 mg/mL (109.53 mM) |
| In vivo | 5% DMSO+40% PEG 300+ddH2O | 9 mg/mL |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 13.05 mL | 65.27 mL | 130.55 mL |
| 0.5 mM | 2.61 mL | 13.05 mL | 26.11 mL |
| 1 mM | 1.31 mL | 6.53 mL | 13.05 mL |
| 5 mM | 0.26 mL | 1.31 mL | 2.61 mL |
*The above data is based on the productmolecular weight 766.0 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
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