CP-868388 free base |
| Katalog-Nr.GC60113 |
Die freie Base CP-868388 ist ein potenter, selektiver und oral aktiver PPARα-Agonist mit einem Ki-Wert von 10,8 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 702681-67-2
Sample solution is provided at 25 µL, 10mM.
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CP-868388 free base is a potent, selective and orally active PPARα agonist with a Ki value of 10.8 nM. CP-868388 free base has little or no affinity for PPARβ (Ki of 3.47 μM) and PPARγ. CP-868388 free base has hypolipidemic and anti-inflammatory actions[1].
CP-868388 (0-1 mM) displays robust and dose-dependent recruitment of SRC-1 (EC50 of 4.7 nM) and PGC-1α peptide[1].CP-868388 demonstrate robust and selective transcriptional activation of PPARα with an EC50 of 18 nM in HepG2 cells[1].
CP-868388 (0-3 mg/kg; oral gavage; once daily; for 2 days; male B6/CBF1J mice) treatment shows a robust and highly significant decrease in circulating plasma triglycerides. Triglyceride lowering is dose-dependent with the greatest efficacy achieved at the 3.0 mg/kg dose, with triglyceride decreases of ~50%[1]. Animal Model: Male B6/CBF1J mice[1]
[1]. Christopher D Kane, et al. Molecular characterization of novel and selective peroxisome proliferator-activated receptor alpha agonists with robust hypolipidemic activity in vivo. Mol Pharmacol. 2009 Feb;75(2):296-306.
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