GlpBio

Encequidar mesylate (HM30181 (mesylate))

目录号: GC33185纯度: >98.00%同义词: HM30181 mesylate; HM30181A mesylate

HM30181 mesylate salt, a tetrazole derivative, is known as a P-glycoprotein inhibitor that has inhibitory activities on multidrug resistance in cancer cells.

Encequidar mesylate (HM30181 (mesylate))
Cas No.: 849675-87-2
规格价格库存数量操作
1mg¥196.00现货
1
5mg¥462.00现货
1
10mg¥637.00现货
1
50mg¥2,030.00现货
1
100mg¥3,080.00现货
1
10mM (in 1mL DMSO)¥550.00现货
1
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产品描述 Description

HM30181 mesylate salt, a tetrazole derivative, is known as a P-glycoprotein inhibitor that has inhibitory activities on multidrug resistance in cancer cells[1,5]. HM30181 has a strong inhibitory effect on MDR1-mediated paclitaxel transport in membrane vesicles. The IC50 value of HM30181 is 0.63 nM[2].

HM30181(10-10M-10-4M;5 min; 37℃) is an effective inhibitor of MDR1in 293FRT-MDR1 cells[2]. The survival inhibition rates of 0.1 nM and 1 nM Encequidar (HM30181) were 20% and 42% respectively, at 100 nM and 1000 nM NSC 125973[3].

HM30181 can significantly improve the bioavailability of oral paclitaxel. In the xenograft model in nude mice, oral co-administration of paclitaxel and HM30181 effectively inhibited tumor growth [2,4].

References:
[1]. Bauer F, Wanek T, 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. doi: 10.1016/j.ejphar.2012.09.013. Epub 2012 Sep 26. PMID: 23022332; PMCID: PMC3690544.
[2]. J.O. Kwak, S.H. Lee, et,al. Selective inhibition of MDR1 (ABCB1) by HM30181 increases oral bioavailability and therapeutic efficacy of paclitaxel
[3]. Joo KM, Song SY, 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. PMID: 18813783.
[4]. Kim JC, Kim KS, 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. doi: 10.1016/j.ijpharm.2016.04.034. Epub 2016 Apr 19. PMID: 27106527.
[5]. J.O. Lee, Y.S. Youn, et,al. Development of poly(lactic-co-glycolic acid) microparticles with pH-sensitive drug release behaviors. J. Pharm. Invest., 45 (2) (2015), pp. 151-156

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

293FRT-MDR1 cells

Preparation Method

The inhibitory activities of HM30181 were measured using the ATPase assay kit. The purified membrane vesicles were diluted to 0.1 µg/µL with assay mix and a 40-µL volume of diluted membrane suspension was loaded into each well of a 96-well microplate. One µL of the tested compound dissolved in dimethylsulfoxide (DMSO) with or without Na-orthovanadate (600 mM) was added to the membrane suspension. The same volume of DMSO was added to the control wells. The mixtures were pre-incubated at 37¡栦or 10 min and the reaction was started by addition of 10 µL Mg-ATP (200 mM). After a 10-min incubation at 37¡欠the inorganic phosphate (Pi) released was determined colorimetrically. The absorbance at 600 nm was read in a microplate reader, and the concentration of liberated Pi was calculated from the calibration curve.

Reaction Conditions

10-10M-10-4M;5 min; 37℃

Applications

HM30181 has a strong inhibitory effect on MDR1-mediated paclitaxel transport in membrane vesicles. The IC50 value of HM30181 is 0.63 nM.
Animal experiment [2]:

Animal models

Male Sprague Dawley rats aged 8 weeks

Preparation Method

Rats were housed under standard husbandry conditions. Rat plasma samples were collected after oral (p.o.) administration of paclitaxel with or without HM30181.

Dosage form

10mg/kg; p.o;0-25hr

Applications

HM30181 can significantly improve the bioavailability of oral paclitaxel.

References:

[1]. J.O. Kwak, S.H. Lee, et,al. Selective inhibition of MDR1 (ABCB1) by HM30181 increases oral bioavailability and therapeutic efficacy of paclitaxel

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
849675-87-2
同义词
HM30181 mesylate; HM30181A mesylate
SMILES
O=C(C1=CC(C2=CC=CC=C2O1)=O)NC3=CC(OC)=C(OC)C=C3C4=NN(C5=CC=C(CCN6CC7=C(C=C(OC)C(OC)=C7)CC6)C=C5)N=N4.CS(=O)(O)=O
分子式
C39H40N6O10S
分子量
784.83 g/mol
溶解性
DMSO : 25 mg/mL (31.85 mM; Need ultrasonic)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol