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格拉非宁盐酸盐 /Glafenine HCl {[allProObj[0].p_purity_real_show]}

货号:A177288 同义名: 格拉非宁盐酸盐 / Glafenin hydrochloride;Glafenine hydrochloride Ambeed 开学季,买赠积分,赢豪礼

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

Glafenine HCl 化学结构 CAS号:65513-72-6
Glafenine HCl 化学结构
CAS号:65513-72-6
Glafenine HCl 3D分子结构
CAS号:65513-72-6
Glafenine HCl 化学结构 CAS号:65513-72-6
Glafenine HCl 3D分子结构 CAS号:65513-72-6
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Glafenine HCl 纯度/质量文件 产品仅供科研

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Glafenine HCl 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].

Glafenine HCl 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

Glafenine HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.22mL

2.44mL

1.22mL

24.43mL

4.89mL

2.44mL

Glafenine HCl 技术信息

CAS号65513-72-6
分子式C19H18Cl2N2O4
分子量 409.263
别名 格拉非宁盐酸盐 ;Glafenin hydrochloride;Glafenine hydrochloride
运输蓝冰
存储条件

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 40 mg/mL(97.74 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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