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CAS No.: 65513-72-6

Glafenine HCl/盐酸格拉芬宁 Catalog No. CSN21978

Synonyms: Glafenin hydrochloride

Glafenine hydrochloride is a non-narcotic analgesic and non-steroidal anti-inflammatory drug and an ABCG2 inhibitor with an IC50 of 3.2 μM.

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技术信息

生物活性

描述Glafenine HCl is a non-narcotic analgesic and non-steroidal anti-inflammatory drug. It is an ABCG2 inhibitor with an IC50 of 3.2 μM^[1]. Glafenine increased the surface expression of Delta Phe508-CFTR in baby hamster kidney (BHK) cells to approximately 40% of that observed for wild-type CFTR, comparable with the known CFTR corrector (VRT-325). Incubating polarized CFBE41o- monolayers and intestines isolated from mutant CFTR mice with glafenine increases the short-circuit current response to forskolin and genistein. Treatment with glafenine also partially restores total salivary secretion^[2]. Glafenine hydrochloride inhibits the proliferation and clonogenic activity of haSMCs and ECs in a dose-dependent manner. A block in the G2/M phase and a reduction in the G1 phase occurr. The migratory ability of haSMCs is impaired in a dose-dependent manner and the extracellular matrix protein tenascin is reduced^[3]. Glafenine induced the unfolded protein response (UPR) and inflammatory pathways in IECs (Intestinal epithelial cell), leading to delamination. Glafenine-induced inflammation was augmented by microbial colonization and associated with changes in intestinal and environmental microbiotas. IEC shedding was a UPR-dependent protective response to Glafenine that restricts inflammation and promotes animal survival^[4].
参考文献

[1] Zhang Y, Byun Y, Ren YR, Liu JO, Laterra J, Pomper MG. Identification of inhibitors of ABCG2 by a bioluminescence imaging-based high-throughput assay. Cancer Res. 2009 Jul 15;69(14):5867-75
[2] Robert R, Carlile GW, Liao J, Balghi H, Lesimple P, Liu N, Kus B, Rotin D, Wilke M, de Jonge HR, Scholte BJ, Thomas DY, Hanrahan JW. Correction of the Delta phe508 cystic fibrosis transmembrane conductance regulator trafficking defect by the bioavailable compound glafenine. Mol Pharmacol. 2010 Jun;77(6):922-30
[3] Schöber W, Tran QB, Muringaseril M, Wiskirchen J, Kehlbach R, Rodegerdts E, Wiesinger B, Claussen CD, Duda SH. Impact of glafenine hydrochloride on human endothelial cells and human vascular smooth muscle cells: a substance reducing proliferation, migration and extracellular matrix synthesis. Cell Biol Int. 2003;27(12):987-96
[4] Espenschied ST, Cronan MR, Matty MA, Mueller O, Redinbo MR, Tobin DM, Rawls JF. Epithelial delamination is protective during pharmaceutical-induced enteropathy. Proc Natl Acad Sci U S A. 2019 Aug 20;116(34):16961-16970

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4434 mL
- 12.2171 mL
- 24.4342 mL
- 5 mM
- 0.4887 mL
- 2.4434 mL
- 4.8868 mL
- 10 mM
- 0.2443 mL
- 1.2217 mL
- 2.4434 mL

技术信息

CAS号

65513-72-6

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H18Cl2N2O4

运输

蓝冰

分子量

409.26

别名

Glafenin hydrochloride

溶解度

DMSO	62.5 mg/mL (152.7 mM)
Water	insoluble

动物实验配方

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