2097125-58-9
Chemical Structure
Encequidar mesylate hydrochloride
Synonym(s): HM30181 mesylate hydrochloride; HM30181A mesylate hydrochloride
- CAS No.: 2097125-58-9
- Formula:C39H42N6O11S
- Molecular Weight:802.85
IUPAC Name: N-(2-(2-(4-(2-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)phenyl)-2H-tetrazol-5-yl)-4,5-dimethoxyphenyl)-4-oxo-4H-chromene-2-carboxamide methanesulfonate hydrate
InChIKey: DGJLRUWQERZYGC-UHFFFAOYSA-N
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.O=S(O)(C)=O.O
Biological Activity: Encequidar (HM30181) mesylate hydrochloride is a potent and selective inhibitor of P-glycoprotein (MDR1). Encequidar mesylate hydrochloride improves anti-tumor efficacy of Paclitaxel (HY-B0015) in mouse tumor models[1][2][3].
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Encequidar mesylate hydrochloride | Encequidar (HM30181) mesylate hydrochloride is a potent and selective inhibitor of P-glycoprotein (MDR1). Encequidar mesylate hydrochloride improves anti-tumor efficacy of Paclitaxel (HY-B0015) in mouse tumor models. | |||||||||||||||||||||
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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]. 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]
- [3]. McCaw ZR, et al. Assessing the Clinical Utility of Oral Paclitaxel Plus Encequidar Versus Intravenous Paclitaxel in Patients With Metastatic Breast Cancer. J Clin Oncol. 2023 Feb 20;41(6):1323. [Content Brief]
