CP671305CAS号： 445295-04-5分子式： C23H19FN2O7分子量： 454.40描述纯度储存/保存方法In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
CP671305 is a potent, orally active, selective inhibitor of phosphodiesterase-4-D, and possesses high activities.
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| 纯度 |
98%
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| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 生物活性 | |
| In vitro(体外研究) |
CP-671,305 is identified as a substrate of MRP2 and BCRP, but not MDR1. CP-671,305 is a substrate of human OATP2B1 with a high affinity (Km=4 μM) but not a substrate for human OATP1B1 or OATP1B3. CP-671,305 displays high affinity (Km=12 μM) for rat hepatic Oatp1a4. CP-671,305 does not exhibit competitive inhibition of the five major cytochrome P450 enzymes, namely CYP1A2, 2C9, 2C19, 2D6 and 3A4 (IC50s > 50 μM). Likewise, no time-dependent inactivation of the five major cytochrome P450 enzymes is discernible with CP-671,305.
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| In vivo(体内研究) |
CP-671,305 is identified as a substrate of MRP2 and BCRP, but not MDR1. CP-671,305 is a substrate of human OATP2B1 with a high affinity (Km=4 μM) but not a substrate for human OATP1B1 or OATP1B3. CP-671,305 displays high affinity (Km=12 μM) for rat hepatic Oatp1a4. CP-671,305 does not exhibit competitive inhibition of the five major cytochrome P450 enzymes, namely CYP1A2, 2C9, 2C19, 2D6 and 3A4 (IC50s > 50 μM). Likewise, no time-dependent inactivation of the five major cytochrome P450 enzymes is discernible with CP-671,305.
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分子结构图
