Glafenine-hydrochloride-Glafenin-hydrochloride-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGlafenine hydrochlorideCat. No.: HY-B1153ACAS No.: 65513-72-6Synonyms: Glafenin hydrochloride分式: CHClNO分量: 409.26作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 60 mg/

2、mL (146.61 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4434 mL 12.2172 mL 24.4343 mL5 mM 0.4887 mL 2.4434 mL 4.8869 mL10 mM 0.2443 mL 1.2217 mL 2.4434 mL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，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Glafenine hydrochloride种醉性痛剂

3、和甾体抗炎药物。它是ABCG2抑制剂，IC50值为3.2 M。IC50 & Target IC50: 3.2 M (ABCG2) 1体外研究Glafenine increases the surface expressionof mutant CFTR in baby hamster kidney (BHK) cells to 40% of1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEthat observed for wild-type CFTR 2. Glafenine hydrochloride inhibits the prolife

4、ration and clonogenic activityof haSMCs and ECs in a dose-dependent manner. A block in the G2/M phase and a reduction in the G1phase occurr. The migratory ability of haSMCs is impaired in a dose-dependent manner and the extracellularmatrix protein tenascin is reduced 3.体内研究 Glafenine injection (25 m

5、g/kg i.v.) shows enhanced BLI signal in mice with an average of 2.9-fold signalenhancement over the control. Glafenine causes increases in BLI signal of up to 11.6- and 17.4-fold in twoseparate HEK293/ABCG2/fLuc xenografts in the same mouse compared to the signals generated by thosexenografts immedi

6、ately before injection 1. Incubating polarized CFBE41o- monolayers and intestinesisolated from mutant CFTR mice with glafenine increases the short-circuit current response to forskolin andgenistein. Treatment with glafenine also partially restores total salivary secretion 2. Glafenine-treatedzebrafi

7、sh shows evidence of endoplasmic reticulum and mitochondrial stress, with disrupted intestinalarchitecture and halted cell stress responses, alongside accumulation of apoptotic intestinal epithelial cells inthe lumen 4.PROTOCOLCell Assay 3 Glafenine hydrochloride is added to the culture medium of th

8、e smooth muscle cells at three concentrations(10 M, 50 M, 100 M). After 4 days of treatment, cells are harvested and the absolute cell number iscounted 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: HEK293/empty/fLuc and HEK293/ABCG2/fLu

9、c cells are implanted subcutaneously into opposite flanksAdministration 1 of female nude mice. Five mice are implanted to generate 10 ABCG2-overexpressing xenografts and fivecontrols. Animals are imaged after D-luciferin administration, which is followed by a bolus injection of a singledose of glafe

10、nine (25 mg/kg) and continued imaging 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Zhang Y, et al. Identification of inhibitors of ABCG2 by a bioluminescence imaging-based high-throughput assay. Cancer Res. 2009 Jul15;69(14):5867-75.2.

11、 Robert R, et al. Correction of the Delta phe508 cystic fibrosis transmembrane conductance regulator trafficking defect by thebioavailable compound glafenine. Mol Pharmacol. 2010 Jun;77(6):922-30.3. Sch?ber W, et al. Impact of glafenine hydrochloride on human endothelial cells and human vascular smo

12、oth muscle cells: a substancereducing proliferation, migration and extracellular matrix synthesis. Cell Biol Int. 2003;27(12):987-96.4. Goldsmith JR, et al. Glafenine-induced intestinal injury in zebrafish is ameliorated by -opioid signaling via enhancement of Atf6-dependent cellular stress responses. Dis Model Mech. 2013 Jan;6(1):146-59.McePdfHeightCaution: