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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,520 | 6-8 weeks | |
50 mg | $1,980 | 6-8 weeks | |
100 mg | $2,500 | 6-8 weeks |
Description | 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. |
Targets&IC50 | BCRP:0.6 μM |
In vitro | ML753286 shows IC50 values of >30, 0.6, and 39.0 μM for the inhibition of P-gp-, BCRP-, and OATP mediated transport, respectively. |
In vivo | 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 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. |
Molecular Weight | 355.43 |
Formula | C20H25N3O3 |
Cas No. | 1699720-89-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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