LY-402913

SKU: orb1700028

Description

LY-402913 is a potent and selective small molecule inhibitor of multidrug resistance-associated protein 1 (MRP1/ABCC1). It is a valuable research tool for studying MRP1-mediated drug efflux and chemoresistance in both cellular assays and animal models.

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 334970-65-9
• MW: 533.96
• Purity: >99.99% (May vary between batches)
• Formula: C₂₈H₂₄ClN₃O₆
• SMILES: O=C1N(C=2C(C3=C1C(C)=NO3)=C(Cl)C=CC2)C4=CC(CC(NC5=CC(OC)=C(OC)C(OC)=C5)=O)=CC=C4
• Target: Others,MRP,P-gp
• Solubility: DMSO:50 mg/mL (93.64 mM)

Bioactivity

• In Vivo:
  When dosed in combination with the oncolytic MRP1 substrate vincristine, LY-402913 delays the growth of MRP1-overexpressing tumors in vivo.
• In Vitro:
  LY-402913 inhibits MRP1 and reverses drug resistance to MRP1 substrates, such as doxorubicin, in HeLa-T5 cells (EC50=0.90 μM), while showing no inherent cytotoxicity. LY-402913 inhibits ATP-dependent, MRP1-mediated LTC4 uptake into membrane vesicles prepared from the MRP1-overexpressing HeLa-T5 cells (EC50=1.8 μM). LY-402913 also shows selectivity (∼22-fold) against the related transporter, P-glycoprotein, in HL60/Adr and HL60/Vinc cells.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LY 402913, LY402913, LY-402913, MRP1

Compound Identifiers

PubChem CID

59119386