Bioactivity | 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]. | ||||||||||||
Invitro | 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]. | ||||||||||||
In Vivo | 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: | ||||||||||||
Name | CP-868388 free base | ||||||||||||
CAS | 702681-67-2 | ||||||||||||
Formula | C26H33NO5 | ||||||||||||
Molar Mass | 439.54 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |