CP-868388 free base

Research use only, not for human use.

CP-868388 free base (CP-868388) is an orally active, potent and selective PPARα agonist with hypolipidemic and anti-inflammatory activity for the study of dyslipidemia.

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.

CP-868388 (0-1 mM) displays robust and dose-dependent recruitment of SRC-1 (EC50 of 4.7 nM) and PGC-1α peptide.CP-868388 demonstrate robust and selective transcriptional activation of PPARα with an EC50 of 18 nM in HepG2 cells.

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%.Animal Model:Male B6/CBF1J mice Dosage:0 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg Administration:Oral gavage; once daily; for 2 days Result:Demonstrated a robust and highly significant decrease in circulating plasma triglycerides.

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Metabolic Enzyme/Protease

PPAR

PPAR

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702681-67-2

439.54

C26H33NO5

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (284.39 mM; Ultrasonic )

CC(C)c1ccc(COC(=O)N2CCC[C@H](C2)c2cccc(OC(C)(C)C(O)=O)c2)cc1

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(-20℃)

With Ice Pack

≥ 2 years