Encequidar mesylate monohydrate

  Cat. No.:  DC70386   Featured
Chemical Structure
2097125-58-9
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Field of application
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.
Cas No.: 2097125-58-9
Chemical Name: HM-30181 mesylate monohydrate
Synonyms: TCA.MSA;Encequidar mesylate;FM0F74;HM 30181A;XRZ6538A8R;Encequidar mesylate (USAN);Encequidar mesylate monohydrate;HM30181 mesylate monohydrate;D11783;4H-1-Benzopyran-2-carboxamide, N-(2-(2-(4-(2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl)phenyl)-2H-tetrazol-5-yl)-4,5-dimethoxyphenyl)-4-oxo-, methanesulfonate, hydrate (1:1:1);HM-30181 mesylate monohydrate
SMILES: S(C([H])([H])[H])(=O)(=O)O[H].O(C([H])([H])[H])C1=C(C([H])=C2C(=C1[H])C([H])([H])N(C([H])([H])C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])N1N=NC(C3=C([H])C(=C(C([H])=C3N([H])C(C3=C([H])C(C4=C([H])C([H])=C([H])C([H])=C4O3)=O)=O)OC([H])([H])[H])OC([H])([H])[H])=N1)C([H])([H])C2([H])[H])OC([H])([H])[H].O([H])[H]
Formula: C39H42N6O11S
M.Wt: 802.8494
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC70386 Encequidar mesylate monohydrate 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.
DC1102 Tariquidar (XR9576) Tariquidar (XR9576) is a potent and selective noncompetitive inhibitor of P-glycoprotein with Kd of 5.1 nM.
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