DC Chemicals Limited
China
Product Name: HM30181 mesylate (Encequidar mesylate)
Price: $500.0/100mg $1000.0/250mg $2000.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

849675-87-2

849675-87-2 structure

849675-87-2 structure

Name: HM30181 mesylate (Encequidar mesylate)
Chemical Name: HM30181 mesylate
CAS Number: 849675-87-2
Molecular Formula: C₃₉H₄₀N₆O₁₀S
Molecular Weight: 784.834
Catalog: Signaling Pathways Membrane Transporter/Ion Channel P-glycoprotein
Create Date: 2019-01-20 19:23:21
Modify Date: 2024-01-12 20:02:56
HM30181 mesylate is a competitive and potent P-glycoprotein inhibitor.

Name	HM30181 mesylate
Synonyms	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 (1:1) Encequidar Mesylate N-[2-(2-{4-[2-(6,7-Dimethoxy-3,4-dihydro-2(1H)-isoquinolinyl)ethyl]phenyl}-2H-tetrazol-5-yl)-4,5-dimethoxyphenyl]-4-oxo-4H-chromene-2-carboxamide methanesulfonate (1:1) HM-30181 MESYLATE

Description	HM30181 mesylate is a competitive and potent P-glycoprotein inhibitor.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein Research Areas >> Cancer
Target	P-glycoprotein[1][2].
In Vitro	Compared with control (0 nM HM30181A), paclitaxel potently inhibits the survival of K1735 cells by about 65% at 100 nM and 72% at 1000 nM in a dose-dependent manner. HM30181A does not make any significant changes in the survival of K1735 cells. In contrast, bEnd.3 cells do not show any decreases in survival by the paclitaxel treatment without HM30181A. However, treatment of 0.1 or 1 nM HM30181A lead to 20 and 42% inhibition of survival at the 100 nM and 1000 nM paclitaxel treatment, respectively[2].
In Vivo	The plasma concentrations of HM30181M are higher for the simultaneous administration with the microcapsule than with the powder; providing significant differences from 1 to 2 h (p < 0.05). The microcapsule has about a 1.7-fold faster Tmax and a 1.6-fold higher AUC value compared with the powder (2.5±0.6 vs. 4.3±0.9 h; 107.7±20.1 vs. 64.3±18.0 h ng/mL). The faster and overall improved absorption of HM30181M in microcapsule form might be due to the remarkable enhancement of the aqueous solubility and dissolution resulting from its crystalline conversion to the amorphous form and particle size reduction[1].
Animal Admin	Rats[1] The cannulised rats are divided into four groups, each comprises of 6 rats. HM30181 M powder or HM30181M- loaded microcapsules are enclosed in hard capsules. One group of rats is dosed orally with paclitaxel solution only, at a drug dose of 20 mg/kg. The rats in the other two groups are administered paclitaxel solution at a drug dose of 20 mg/kg simultaneously with either capsules containing HM30181 M powder or microcapsules (equivalent to 20 mg/kg HM30181 M)[1].
References	[1]. Kim JC, et al. Effect of HM30181 mesylate salt-loaded microcapsules on the oral absorption of paclitaxel as a novel P-glycoprotein inhibitor. Int J Pharm. 2016 Jun 15;506(1-2):93-101. [2]. Joo KM, et al. Response of brain specific microenvironment to P-glycoprotein inhibitor: an important factor determining therapeutic effect of P-glycoprotein inhibitor on brain metastatic tumors. Int J Oncol. 2008 Oct;33(4):705-12.

Molecular Formula	C₃₉H₄₀N₆O₁₀S
Molecular Weight	784.834
Exact Mass	784.252686