Chemical Structure : Encequidar
CAS No.: 849675-66-7
Catalog No.: PC-73218Not For Human Use, Lab Use Only.
Encequidar (HM30181) is a potent selective inhibitor of MDR1 (ABCB1, P-gp) with IC50 of 0.63 nM.
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Encequidar (HM30181) is a potent selective inhibitor of MDR1 (ABCB1, P-gp) with IC50 of 0.63 nM.
Encequidar (HM30181) effectively blocked transepithelial transport of paclitaxel in MDCK monolayers.
Encequidar (HM30181) does not inhibit MRP1 (ABCC1), MRP2 (ABCC2), and MRP3 (ABCC3), and partially inhibited BCRP (ABCG2) only at very high concentrations.
Oral co-administration of paclitaxel and HM30181 showed a tumor-inhibitory strength equal or superior to that of intravenous paclitaxel in the xenograft model in nude mice.
M.Wt | 688.741 | |
Formula | C38H36N6O7 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
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 |
1. Kim TE, et al. Br J Clin Pharmacol. 2014 Sep;78(3):556-64.
2. Bauer F, et al. Eur J Pharmacol. 2012 Dec 5;696(1-3):18-27.
3. Kwak JO, et al. Eur J Pharmacol. 2010 Feb 10;627(1-3):92-8.
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