CP-868388 free base

Names

[ Name ]:
CP-868388 free base

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> PPAR

Research Areas >> Inflammation/Immunology

Research Areas >> Metabolic Disease

Research Areas >> Neurological Disease

[Target]

hPPARα:10.8 nM (Ki)

hPPARγ:3.47 μM (Ki)

[In Vitro]

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: Male B6/CBF1J mice[1] 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.

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₆H₃₃NO₅

[ Molecular Weight ]:
439.54400

[ Exact Mass ]:
439.23600

[ PSA ]:
76.07000

[ LogP ]:
5.50610

Safety Information

[ Symbol ]:

GHS06, GHS09

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301-H410

[ Precautionary Statements ]:
P273-P301 + P310-P501

[ RIDADR ]:
UN 2811 6.1 / PGIII

Related Compounds

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