Gemcabene

Names

[ Name ]:
Gemcabene

[Synonym ]:
Gemcabene
UNII-B96UX1DDKS

Biological Activity

[Description]:

Gemcabene (PD-72953), a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) and lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP), exerting anti-inflammatory activity[1][2][3].

[Related Catalog]:

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

Research Areas >> Metabolic Disease

[In Vitro]

Gemcabene calcium (PD-72953 calcium) significantly downregulates hepatic mRNA markers of inflammation (TNF-α, MCP-1, MIP-1β, CCR5, CCR2, NF-κB), lipogenesis and lipid modulation (ApoC-III, ACC1, ADH-4, Sulf-2), and fibrosis (TIMP-1 and MMP-2)[3].

[References]

[1]. Mandema JW, et al. Model-based development of gemcabene, a new lipid-altering agent. AAPS J. 2005 Oct 7;7(3):E513-22.

[2]. Srivastava RAK, et al. Gemcabene, a First-in-Class Hypolipidemic Small Molecule in Clinical Development, Attenuates Osteoarthritis and Pain in Animal Models of Arthritis and Pain. Front Pharmacol. 2018 May 11;9:471.

[3]. Oniciu DC, et al. Gemcabene downregulates inflammatory, lipid-altering and cell-signaling genes in the STAM™ model of NASH. PLoS One. 2018 May 30;13(5):e0194568.

Chemical & Physical Properties

[ Density]:
1.048g/cm3

[ Boiling Point ]:
453.6ºC at 760mmHg

[ Molecular Formula ]:
C₁₆H₃₀O₅

[ Molecular Weight ]:
302.40600

[ Flash Point ]:
156.7ºC

[ Exact Mass ]:
302.20900

[ PSA ]:
83.83000

[ LogP ]:
3.56520

[ Vapour Pressure ]:
1.72E-09mmHg at 25°C

[ Index of Refraction ]:
1.473

[ Storage condition ]:
2-8℃

Synthetic Route

Click to get detail synthetic route

Related Compounds

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