产品
编 号：F203424
分子式：C20H25N3O3
分子量：355.43
分子式：C20H25N3O3
分子量：355.43
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CAS No: 1699720-89-2
产品详情
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.
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.Animal Model:Male Bcrp KO (Abcg2?/?) and WT (Wistar) Rats
Dosage:25- or 50-mg/kg (PO); 10 or 20 mg/kg (IV) (Pharmacokinetic Study)
Administration:PO or IV; 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, and 24 hours
Result: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.
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.
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.
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.Animal Model:Male Bcrp KO (Abcg2?/?) and WT (Wistar) Rats
Dosage:25- or 50-mg/kg (PO); 10 or 20 mg/kg (IV) (Pharmacokinetic Study)
Administration:PO or IV; 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, and 24 hours
Result: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.
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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