Cas No.: | 183293-82-5 |
Chemical Name: | 6-(5-carboxy-5-methylhexoxy)-2,2-dimethylhexanoic acid |
Synonyms: | PD-72953;PD72953 |
SMILES: | C(O)(=O)C(C)(C)CCCCOCCCCC(C(O)=O)(C)C |
Formula: | C16H30O5 |
M.Wt: | 302.411 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Publication: | [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. |
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]. |
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. |