Encequidar (hydrochloride)

Encequidar hydrochloride (HM30181 hydrochloride) is an oral P-glycoprotein (P-gp) inhibitor with the activity of enhancing the oral bioavailability of P-gp substrate drugs. Encequidar shows the highest potency among various MDR1 inhibitors, with IC50=0.63nM. Encequidar effectively blocks the transepithelial transport of paclitaxel in MDCK monolayer cells, with IC50=35.4nM[1].

Product Specifications

CAS Number

[849675-88-3]

Product Name Alternative

HM30181 (hydrochloride) ; HM30181A (hydrochloride)

UNSPSC

12352005

Target

P-glycoprotein

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Others

Assay Protocol

https://www.medchemexpress.com/Encequidar_hydrochloride.html

Smiles

O=C1C=C(C(NC2=CC(OC)=C(C=C2C3=NN(C4=CC=C(CCN5CC6=CC(OC)=C(C=C6CC5)OC)C=C4)N=N3)OC)=O)OC7=C1C=CC=C7.Cl

Molecular Formula

C38H37ClN6O7

Molecular Weight

725.19

References & Citations

[1]Bauer F, et al. Interaction of HM30181 with P-glycoprotein at the murine blood-brain barrier assessed with positron emission tomography. Eur J Pharmacol. 2012 Dec 5;696 (1-3) :18-27.|[2]Kim TE, et al. Effects of HM30181, a P-glycoprotein inhibitor, on the pharmacokinetics and pharmacodynamics of loperamide in healthy volunteers. Br J Clin Pharmacol. 2014 Sep;78 (3) :556-64.|[3]Oral docetaxel plus encequidar - a phase 1 clinical trial