[CAS NO. 183293-82-5] Gemcabene
PRODUCTS SPECIFICATIONS [183293-82-5]
DESCRIPTION [183293-82-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 302.41 |
| Molecular Formula | C16H30O5 |
| SMILES | O=C(O)C(C)(C)CCCCOCCCCC(C)(C)C(O)=O |
Summary
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02944383 | NeuroBo Pharmaceuticals Inc. |
Severe Hypertriglyceridemia|Mixed Dyslipidaemia
|
December 2016 | Phase 2 |
| NCT02591836 | NeuroBo Pharmaceuticals Inc. |
Hypercholesterolemia
|
January 2003 | Phase 2 |
| NCT02587364 | NeuroBo Pharmaceuticals Inc. |
Hypercholesterolemia
|
April 1999 | Phase 1 |
| NCT02585869 | NeuroBo Pharmaceuticals Inc. |
Hypercholesterolemia|Hypertriglyceridemia
|
December 1999 | Phase 2 |
| NCT02587416 | NeuroBo Pharmaceuticals Inc. |
Hypercholesteremia
|
November 2002 | Phase 1 |
| NCT02587390 | NeuroBo Pharmaceuticals Inc. |
Hypercholesterolemia
|
May 2000 | Phase 1 |
| NCT02722408 | NeuroBo Pharmaceuticals Inc. |
Hypercholesteremia
|
June 2016 | Phase 2 |
| NCT02571257 | NeuroBo Pharmaceuticals Inc. |
Hypercholesterolemia
|
August 2000 | Phase 2 |
| NCT03508687 | Elif Oral|University of Michigan |
Familial Partial Lipodystrophy|Hypertriglyceridemia|Fatty Liver|NASH - Nonalcoholic Steatohepatitis
|
March 13, 2018 | Phase 1|Phase 2 |
| NCT02586168 | NeuroBo Pharmaceuticals Inc. |
Insulin Sensitivity
|
July 2001 | Phase 2 |
| NCT03436420 | Emory University|Gemphire Therapeutics |
Non-Alcoholic Fatty Liver Disease
|
March 29, 2018 | Phase 2 |
| NCT02634151 | NeuroBo Pharmaceuticals Inc. |
Hypercholesteremia
|
November 2016 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 330.68 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.3068 mL | 16.5338 mL | 33.0677 mL |
| 5 mM | 0.6614 mL | 3.3068 mL | 6.6135 mL |
| 10 mM | 0.3307 mL | 1.6534 mL | 3.3068 mL |
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.