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CP671305

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Chemical Structure| 445295-04-5 同义名 : -
CAS号 : 445295-04-5
货号 : A723969
分子式 : C23H19FN2O7
纯度 : 99%+
分子量 : 454.405
MDL号 : MFCD31382154
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(231.07 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 CP671305 is a substrate for MRP2 and BCRP, but not for MDR1. It is also a substrate for human OATP2B1, exhibiting high affinity (Km=4 μM), but it is not a substrate for human OATP1B1 or OATP1B3. CP671305 shows high affinity for rat liver Oatp1a4 (Km=12 μM)[1]. CP671305 does not exhibit competitive inhibition for the five major cytochrome P450 enzymes (namely CYP1A2, 2C9, 2C19, 2D6, and 3A4), with IC50 values greater than 50 μM. Likewise, no time-dependent inactivation of these major cytochrome P450 enzymes is observed following treatment with CP671305[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

11.00mL

2.20mL

1.10mL

22.01mL

4.40mL

2.20mL
参考文献

[1]Kalgutkar AS, et al. Role of transporters in the disposition of the selective phosphodiesterase-4 inhibitor (+)-2-[4-({[2-(benzo[1,3]dioxol-5-yloxy)-pyridine-3-carbonyl]-amino}-methyl)-3-fluoro-phenoxy]-propionic acid in rat and human. Drug Metab Dispos. 2007 Nov;35(11):2111-8. Epub 2007 Aug 8.

[2]Kalgutkar AS, et al. Disposition of CP-671, 305, a selective phosphodiesterase 4 inhibitor in preclinical species. Xenobiotica. 2004 Aug;34(8):755-70.