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ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions. ML753286 is an orally active and selective inhibitor of BCRP (IC50: 0.6 μM). It is also stable in plasma across species.
ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions. ML753286 is an orally active and selective inhibitor of BCRP (IC50: 0.6 μM). It is also stable in plasma across species.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | |
50 mg | ¥ 13,800 | 6-8周 | |
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions. ML753286 is an orally active and selective inhibitor of BCRP (IC50: 0.6 μM). It is also stable in plasma across species. |
靶点活性 | BCRP:0.6 μM |
体外活性 | ML753286 shows IC50 values of >30, 0.6, and 39.0 μM for the inhibition of P-gp-, BCRP-, and OATP mediated transport, respectively. |
体内活性 | ML753286 (25- or 50-mg/kg (PO); 10 or 20 mg/kg (IV); 0.083-24 hours) appears to fully suppress Bcrp functions in rats at 25 mg/kg p.o. or at 20 mg/kg i.v. In Bcrp KO rats, pre-administered ML753286(25-mg/kg ; WT rats) and pre-administered ML753286 (50-mg/kg; WT rats), the tmax values in plasma were 1.4, 4.0, and 4.1 hours , respectively. |
分子量 | 355.43 |
分子式 | C20H25N3O3 |
CAS No. | 1699720-89-2 |
密度 | 1.27 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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