ML753286

产品编号 T16113Cas号 1699720-89-2

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

产品编号 T16113Cas号 1699720-89-2

规格	价格	库存
25 mg	¥ 10,600	6-8周
50 mg	¥ 13,800	6-8周
100 mg	¥ 17,500	6-8周

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产品介绍

生物活性

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.