Encequidar hydrochloride
Based on 5 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 849675-88-3
- Formula: C38H37ClN6O7
- Molecular Weight:725.19
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Encequidar hydrochloride
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Biological Activity
Chemical Information
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CAS No. 849675-88-3
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Molecular Weight 725.19
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Formula C38H37ClN6O7
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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
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Synonyms
HM30181 hydrochloride; HM30181A hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Commun
Carbon nano-onion-mediated dual targeting of P-selectin and P-glycoprotein to overcome cancer drug resistance. [Abstract]2021 Jan 12;12(1):312. PMID: 33436622 -
EMBO J
2024 Oct;43(19):4406-4436. PMID: 39160273 -
Crit Rev Anal Chem
A Critical Review on Advancement in Analytical Strategies for the Quantification of Clinically Relevant Biological Transporters. [Abstract]2022;52(7):1557-1571. PMID: 33691566 -
Hepatol Commun
Inhibition of the transmembrane transporter ABCB1 overcomes resistance to doxorubicin in patient-derived organoid models of HCC. [Abstract]2024 May 2;8(5):e0437. PMID: 38696353 -
Drug Metab Dispos
Encequidar is a multispecies gut-restricted P-glycoprotein inhibitor that delineates between intestinal secretion and biliary elimination in animals and predicts human disposition pathways. [Abstract]2026 Jan 16;54(3):100237. PMID: 41655312
Purity & Documentation
References
[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. [Content Brief]
[2]. Oral docetaxel plus encequidar - a phase 1 clinical trial [Content Brief]
[3]. 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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Encequidar hydrochloride Related Classifications
HY-13646B Related Classifications
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