MDL | - |
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Molecular Weight | 355.43 |
Molecular Formula | C20H25N3O3 |
SMILES | COC1=CC=C2C(NC3=C2C[C@]4(N([C@H]3CC(C)C)C([C@@H](NC4=O)C)=O)[H])=C1 |
IC50: 0.6 μM (BCRP) [1]
ML753286 has IC 50 values of >30, 0.6, and 39.0 μM for the inhibition of P-gp-, BCRP-, and OATP mediated transport, respectively [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 t max 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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | Male Bcrp KO (Abcg2−/−) and WT (Wistar) Rats [1] |
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 t max 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. |
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
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4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |