生物活性
Posaconazole主要是CYP3A4的抑制剂，但不抑制其他CYP酶的活性。也是甾醇C14+脱甲基酶抑制剂的抑制剂，IC50为0.25μM。泊沙康唑的终末消除半衰期中位数为15-35小时。
靶点信息
| lanosterol 14α-demethylase | | | | |
| | | | |
化学数据
| 目录号 | A10744 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 700.8 |
| Formula | C37H42F2N8O4 |
| 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. | 171228-49-2 |
| Synonyms | Noxafil |
| SMILES | CC[C@@H]([C@H](C)O)N1C(=O)N(C=N1)C2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(C=C4)OC[C@H]5C[C@](OC5)(CN6C=NC=N6)C7=C(C=C(C=C7)F)F |
溶解度
| In vitro (25°C) | DMSO | 90 mg/mL (128.42 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 1% DMSO+30% polyethylene glycol+1% Tween 80 | 28 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 | 14.27 mL | 71.35 mL | 142.69 mL |
| 0.5 mM | 2.85 mL | 14.27 mL | 28.54 mL |
| 1 mM | 1.43 mL | 7.13 mL | 14.27 mL |
| 5 mM | 0.29 mL | 1.43 mL | 2.85 mL |
*The above data is based on the productmolecular weight 700.8 . 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.
