1. Membrane Transporter/Ion Channel
  2. BCRP
  3. ML753286

ML753286 

Cat. No.: HY-116494
Handling Instructions

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.

For research use only. We do not sell to patients.

ML753286 Chemical Structure

ML753286 Chemical Structure

CAS No. : 1699720-89-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 766 In-stock
Estimated Time of Arrival: December 31
1 mg USD 550 In-stock
Estimated Time of Arrival: December 31
5 mg USD 980 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

IC50 & 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.
Molecular Weight

355.43

Formula

C₂₀H₂₅N₃O₃

CAS No.

1699720-89-2

SMILES

COC1=CC=C2C(NC3=C2C[[email protected]]4(N([[email protected]]3CC(C)C)C([[email protected]@H](NC4=O)C)=O)[H])=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

ML753286ML 753286ML-753286BCRPBreast cancer resistance proteinABCG2Inhibitorinhibitorinhibit

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ML753286
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