MCE products for research use only. We do not sell to patients.

Glafenine hydrochloride

MCE China：Glafenine hydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-B1153A

CAS：65513-72-6

Synonyms：Glafenin hydrochloride

Purity：99.25%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Glafenine hydrochloride is a non-narcotic analgesic and non-steroidal anti-inflammatory drug. It is an ABCG2 inhibitor with an IC50 of 3.2 μM. Glafenine can also antagonize the misfolding of SLC4A11 protein.

In Vitro：Glafenine increases the surface expressionof mutant CFTR in baby hamster kidney (BHK) cells to 40% of that observed for wild-type CFTR[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].

In Vivo：Glafenine injection (25 mg/kg i.v.) shows enhanced BLI signal in mice with an average of 2.9-fold signal enhancement over the control. Glafenine causes increases in BLI signal of up to 11.6- and 17.4-fold in two separate HEK293/ABCG2/fLuc xenografts in the same mouse compared to the signals generated by those xenografts immediately before injection[1]. 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-treated zebrafish shows evidence of endoplasmic reticulum and mitochondrial stress, with disrupted intestinal architecture and halted cell stress responses, alongside accumulation of apoptotic intestinal epithelial cells in the lumen[4].

Animal Administration：Mice: HEK293/empty/fLuc and HEK293/ABCG2/fLuc cells are implanted subcutaneously into opposite flanks of female nude mice. Five mice are implanted to generate 10 ABCG2-overexpressing xenografts and five controls. Animals are imaged after D-luciferin administration, which is followed by a bolus injection of a single dose of glafenine (25 mg/kg) and continued imaging[1].

Cell Assay：Glafenine hydrochloride is added to the culture medium of the smooth muscle cells at three concentrations (10 μM, 50 μM, 100 μM). After 4 days of treatment, cells are harvested and the absolute cell number is counted[3].

IC50 & Target：IC50: 3.2 μM (ABCG2)[1] In Vitro Glafenine increases the surface expressionof mutant CFTR in baby hamster kidney (BHK) cells to 40% of that observed for wild-type CFTR[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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Glafenine hydrochloride Related Antibodies

Hot selling product：Mitotane  | DMAT  | Retapamulin  | Synta66  | Benfluorex (hydrochloride)  | Schisantherin A  | Pretomanid  | DTE  | Paroxetine  | Neophytadiene

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides

References：

[1]. Zhang Y, et al. Identification of inhibitors of ABCG2 by a bioluminescence imaging-based high-throughput assay. Cancer Res. 2009 Jul 15;69(14):5867-75.  [Content Brief]

[2]. Robert R, et al. 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.  [Content Brief]

[3]. Schöber W, et al. 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.  [Content Brief]

[4]. Goldsmith JR, et al. Glafenine-induced intestinal injury in zebrafish is ameliorated by μ-opioid signaling via enhancement of Atf6-dependent cellular stress responses. Dis Model Mech. 2013 Jan;6(1):146-59.  [Content Brief]

[5]. Chiu AM, et al. High Throughput Assay Identifies Glafenine as a Corrector for the Folding Defect in Corneal Dystrophy-Causing Mutants of SLC4A11. Invest Ophthalmol Vis Sci. 2015 Dec;56(13):7739-53.  [Content Brief]