Molecular Formula | C19H18Cl2N2O4 |
Molar Mass | 409.26 |
Appearance | neat |
Storage Condition | Inert atmosphere,Room Temperature |
In vitro study | Glafenine increases the surface expressionof mutant CFTR in baby hamster kidney (BHK) cells to 40% of that observed for wild-type CFTR. 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. |
In vivo study | 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. 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. 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. |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
Safety Description | 36 - Wear suitable protective clothing. |
WGK Germany | 3 |
RTECS | CB2687000 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.443 ml | 12.217 ml | 24.434 ml |
5 mM | 0.489 ml | 2.443 ml | 4.887 ml |
10 mM | 0.244 ml | 1.222 ml | 2.443 ml |
5 mM | 0.049 ml | 0.244 ml | 0.489 ml |