CP-868388freebase是一种有效的，选择性的，具有口服活性的PPARα激动剂，Ki值为10.8nM。CP-868388freebase对PPARβ(Ki为3.47μM)和PPARγ几乎没有亲和力，具有降血脂和抗炎作用。
货号:ajcx29240
CAS:702681-67-2
分子式:C26H33NO5
分子量：439.54
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.