Encequidar

SKU: orb1298944

Description

Encequidar (HM30181A) is a selective and potent inhibitor of P-glycoprotein. It is used in research to overcome multidrug resistance in cancer cells, facilitating studies on chemotherapeutic efficacy in both in vitro and in vivo experimental models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 849675-66-7
• MW: 688.73
• Purity: 99.93% (May vary between batches)
• Formula: C₃₈H₃₆N₆O₇
• SMILES: COc1cc2CCN(CCc3ccc(cc3)-n3nnc(n3)-c3cc(OC)c(OC)cc3NC(=O)c3cc(=O)c4ccccc4o3)Cc2cc1OC
• Target: P-gp
• Solubility: DMSO:6.9 mg/mL (10.02 mM)

Bioactivity

• In Vivo:
  HM30181 to inhibit Pgp at the murine BBB. HM30181 was shown to be approximately equipotent with the reference Pgp inhibitor tariquidar in inhibiting rhodamine 123 efflux from CCRF-CEM T cells (IC(50), tariquidar: 8.2 2.0 nM, HM30181: 13.1 2.3 nM). PET scans with the Pgp substrate (R)-[(11)C]verapamil in FVB wild-type mice pretreated i.v. with HM30181 (10 or 21 mg/kg) failed to show significant increases in (R)-[(11)C]verapamil brain uptake compared with vehicle treated animals. PET scans with [(11)C]HM30181 showed low and not significantly different brain uptake of [(11)C]HM30181 in wild-type, Mdr1a/b((-/-)) and Bcrp1((-/-)) mice and significantly, i.e. 4.7-fold (P<0.01), higher brain uptake, relative to wild-type animals, in Mdr1a/b((-/-))Bcrp1((-/-)) mice.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

P-glycoprotein, Pgp, P-gp, P-gp (P-glycoprotein), CD243, Cluster of differentiation 243, ABCB1, Multidrug resistance protein 1, inhibit, HM 30181, HM30181, HM-30181, HM30181A, MDR1, Inhibitor, Encequidar

Compound Identifiers

PubChem CID

11399764