1699720-89-2
1699720-89-2 structure
- Name: ML753286
- Chemical Name: ML753286
- CAS Number: 1699720-89-2
- Molecular Formula: C20H25N3O3
- Molecular Weight: 355.43
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel BCRP
- Create Date: 2019-12-08 17:18:19
- Modify Date: 2024-01-10 12:41:34
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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[1].
| Name | ML753286 |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| Target |
IC50: 0.6 μM (BCRP)[1] |
| In Vitro | ML753286 has IC50 values of >30, 0.6, and 39.0 μM for the inhibition of P-gp-, BCRP-, and OATP mediated transport, respectively[1]. |
| In Vivo | 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[1]. 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 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. |
| References |
| Molecular Formula | C20H25N3O3 |
|---|---|
| Molecular Weight | 355.43 |