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 shows IC50 values of >30, 0.6, and 39.0 μM for the inhibition of P-gp-, BCRP-, and OATP mediated transport, respectively.

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.

1699720-89-2

C20H25N3O3

355.43

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years