CP-868388 free base

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CP-868388 free base 是一种有效的，选择性的，具有口服活性的 PPARα 激动剂，Ki 值为 10.8 nM。CP-868388 free base 对 PPARβ (Ki 为 3.47 μM) 和 PPARγ 几乎没有亲和力，具有降血脂和抗炎作用。

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 中的溶解度 : 125 mg/mL (284.39 mM; 超声助溶 )

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