ML753286 是一种口服活性和选择性 BCRP (抗乳腺癌蛋白) 抑制剂，IC50 为 0.6 μM。 ML753286 在啮齿动物和人类肝脏 S9 组分中具有高渗透性和低至中等清除率，并且在不同物种中都具有血浆稳定性。
| 生物活性 |
ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species. |
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| 体外研究 |
ML753286 has IC50 values of >30, 0.6, and 39.0 μM for the inhibition of P-gp-, BCRP-, and OATP mediated transport, respectively. |
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| 体内研究 |
ML753286 (25- or 50-mg/kg (PO); 10 or 20 mg/kg (IV); 0.083-24 hours) appears to completely inhibit Bcrp functions in rats at 25 mg/kg PO or at 20 mg/kg IV. The tmax values in plasma were 1.4, 4.0, and 4.1 hours in Bcrp KO rats, WT rats pre-administered 25-mg/kg ML753286, and WT rats pre-administered 50-mg/kg ML753286, respectively.
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| 分子式 |
C20H25N3O3
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| 分子量 |
355.43
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| CAS号 |
1699720-89-2
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
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| 科研文献 |
纯度： 98%
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