PEKXWELLWNPUOK-UHFFFAOYSA-N
Encequidar mesylate
CAS: 849675-87-2
Molecular Formula: C39H40N6O10S
PEKXWELLWNPUOK-UHFFFAOYSA-N - Names and Identifiers
| Name | Encequidar mesylate |
| Synonyms | HM30181A mesylate HM30181 (Mesylate) Encequidar mesylate PEKXWELLWNPUOK-UHFFFAOYSA-N Encequidar mesylate (HM-30181 HM30181 mesylate (Encequidar mesylate) |
| CAS | 849675-87-2 |
PEKXWELLWNPUOK-UHFFFAOYSA-N - Physico-chemical Properties
| Molecular Formula | C39H40N6O10S |
| Molar Mass | 784.84 |
| Solubility | Soluble in DMSO, not in water |
| Storage Condition | -20℃ |
| Use | Encequidar, also known as HM-30181, is an oral P-glycoprotein (P-gp) inhibitor developed to enhance the oral bioavailability of P-gp substrate drugs. Encequidar showed the highest potency (IC(50)=0.63nM) among several MDR1 inhibitors, including cycloporin A, XR9576, and GF120918, and effectively blocked transepithelial transport of paclitaxel in MDCK monolayers (IC(50)=35.4nM). Encequidar is currently under clinical trials. |
| Target | P-glycoprotein |
PEKXWELLWNPUOK-UHFFFAOYSA-N - Reference
| Reference Show more | 1: Cha YJ, Lee H, Gu N, Kim TE, Lim KS, Yoon SH, Chung JY, Jang IJ, Shin SG, Yu KS, Cho JY. Sustained Increase in the Oral Bioavailability of Loperamide after a Single Oral Dose of HM30181, a P-glycoprotein Inhibitor, in Healthy Male Participants. Basic Clin Pharmacol Toxicol. 2013 Jul 6. doi: 10.1111/bcpt.12108. [Epub ahead of print] PubMed PMID: 23829508. 2: Bauer F, Wanek T, Mairinger S, Stanek J, Sauberer M, Kuntner C, Parveen Z, Chiba P, Müller M, Langer O, Erker T. 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. PubMed PMID: 23022332; PubMed Central PMCID: PMC3690544. 3: Kim TE, Gu N, Yoon SH, Cho JY, Park KM, Shin SG, Jang IJ, Yu KS. Tolerability and pharmacokinetics of a new P-glycoprotein inhibitor, HM30181, in healthy Korean male volunteers: single- and multiple-dose randomized, placebo-controlled studies. Clin Ther. 2012 Feb;34(2):482-94. doi: 10.1016/j.clinthera.2012.01.003. Epub 2012 Jan 28. PubMed PMID: 22284902. 4: Kwak JO, Lee SH, Lee GS, Kim MS, Ahn YG, Lee JH, Kim SW, Kim KH, Lee MG. Selective inhibition of MDR1 (ABCB1) by HM30181 increases oral bioavailability and therapeutic efficacy of paclitaxel. Eur J Pharmacol. 2010 Feb 10;627(1-3):92-8. doi: 10.1016/j.ejphar.2009.11.008. Epub 2009 Nov 10. PubMed PMID: 19903471. |
PEKXWELLWNPUOK-UHFFFAOYSA-N - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 0 ml | 0 ml | 0 ml |
| 5 mM | 0 ml | 0 ml | 0 ml |
| 10 mM | 0 ml | 0 ml | 0 ml |
| 5 mM | 0 ml | 0 ml | 0 ml |
Last Update：2024-01-02 23:10:35
Supplier List
Product Name: Encequidar Mesylate Request for quotation
CAS: 849675-87-2
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
CAS: 849675-87-2
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Product Name: Encequidar mesylate Visit Supplier Webpage Request for quotation
CAS: 849675-87-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 849675-87-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Product Name: Encequidar Mesylate Request for quotation
CAS: 849675-87-2
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
CAS: 849675-87-2
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Product Name: Encequidar mesylate Visit Supplier Webpage Request for quotation
CAS: 849675-87-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 849675-87-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History