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Encequidar

Chemical Structure : Encequidar

CAS No.: 849675-66-7

Encequidar (HM 30181)

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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 688.741
Formula C38H36N6O7
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

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

References

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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