Encequidar (hydrochloride)
Product Specifications
UNSPSC Description
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].
Target Antigen
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 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
Shipping Conditions
Room temperature
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-13646B/Encequidar-hydrochloride-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-13646B/
Clinical Information
Phase 2
CAS Number
849675-88-3
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