| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Gemcabene targets multiple pathways involved in lipid metabolism and inflammation. It is described as an activator of PARP and exerts its lipid-lowering effects through mechanisms distinct from statins and fibrates. The compound lowers LDL-C, decreases triglycerides, and raises HDL-C. It also reduces CRP levels, demonstrating anti-inflammatory properties.
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| ln Vitro |
Gemcabene Calcium (PD-72953 Calcium) markedly reduces the expression of mRNA markers associated with liver inflammation (TNF-α, MCP-1, MIP-1β, CCR5, CCR2, NF-κB), adipogenesis, and lipid regulation (ApoC-III, ACC1, ADH-4, Sulf-2) as well as fibrosis (TIMP-1 and MMP-2) [3].
In vitro, Gemcabene has demonstrated lipid-lowering and anti-inflammatory activities. It down-regulates pro-inflammatory pathways and reduces CRP expression. The compound's ability to modulate lipid metabolism and inflammation has been characterized in various cell-based assays. |
| ln Vivo |
In vivo, Gemcabene attenuates osteoarthritis and pain in animal models of arthritis. It has demonstrated potent, efficacious, and durable dose-dependent reductions in lipid levels in preclinical studies. The compound's efficacy in lowering LDL-C and triglycerides while raising HDL-C supports its development for dyslipidemia and related metabolic disorders.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Gemcabene typically involve measuring its effects on lipid metabolism enzymes and inflammatory markers. PARP activation assays may be performed to characterize the compound's mechanism. CRP levels are measured in cell culture supernatants to assess anti-inflammatory activity.
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| Cell Assay |
In vitro cellular assays are performed using hepatocytes or macrophage cell lines. Cells are treated with Gemcabene at various concentrations, and lipid accumulation is assessed by Oil Red O staining or by measuring intracellular cholesterol and triglyceride levels. Inflammatory markers such as CRP, TNF-α, and IL-6 are measured by ELISA to evaluate anti-inflammatory effects.
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| Animal Protocol |
In vivo studies are conducted in animal models of dyslipidemia, such as LDL receptor knockout mice or high-fat diet-fed hamsters. Gemcabene is administered orally at various doses. Serum lipid profiles (total cholesterol, LDL-C, HDL-C, triglycerides) are measured at multiple time points. In models of arthritis, pain behaviors and joint inflammation are assessed.
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| ADME/Pharmacokinetics |
Gemcabene (molecular weight 302.41, formula C₁₆H₃₀O₅) is a small-molecule compound. Its IUPAC name is 6-(5-carboxy-5-methylhexoxy)-2,2-dimethylhexanoic acid. The compound is typically stored at -20°C. Its physicochemical properties support oral bioavailability and once-daily dosing.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies have evaluated Gemcabene in animal models. As a lipid-lowering agent, its toxicity profile is related to effects on lipid metabolism and potential gastrointestinal effects. The compound has demonstrated a manageable safety profile in preclinical studies.
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| 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. |
| Additional Infomation |
Gemcabene is a novel drug that lowers low-density lipoprotein cholesterol (LDL-C) and triglycerides while raising high-density lipoprotein cholesterol (HDL-C). Gemcabene is a dialkyl ether dicarboxylic acid with anti-hyperlipidemic activity. In animal models, Gemcabene increases HDL cholesterol levels and enlarges HDL particle size. Simultaneously, LDL cholesterol, triglyceride, and apolipoprotein C-III levels are also reduced. In human trials, the HDL-lowering effect of Gemcabene was observed only in patients with high triglyceride levels (>200 mg/dL). Drug Indications It has been investigated for the treatment of atherosclerosis, cardiovascular disease, and hyperlipidemia.
Gemcabene (PD-72953) is a first-in-class lipid-lowering agent developed for dyslipidemia and related metabolic disorders. Its mechanism involves lowering LDL-C and triglycerides while raising HDL-C, along with anti-inflammatory effects through CRP reduction. The compound has been investigated for atherosclerosis, diabetes, and NAFLD. Despite promising preclinical and clinical data, Gemcabene has not received regulatory approval for commercial use. |
| Molecular Formula |
C16H30O5
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|---|---|
| Molecular Weight |
302.4064
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| Exact Mass |
302.209
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| CAS # |
183293-82-5
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| Related CAS # |
Gemcabene calcium;209789-08-2
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| PubChem CID |
157692
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| Appearance |
White to off-white solid powder
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| Density |
1.048g/cm3
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| Boiling Point |
453.6ºC at 760mmHg
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| Flash Point |
156.7ºC
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| Vapour Pressure |
1.72E-09mmHg at 25°C
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| Index of Refraction |
1.473
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| LogP |
3.565
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
21
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| Complexity |
302
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(CCCCC(C(=O)O)(C)C)CCCCC(C(=O)O)(C)C
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| InChi Key |
SDMBRCRVFFHJKR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H30O5/c1-15(2,13(17)18)9-5-7-11-21-12-8-6-10-16(3,4)14(19)20/h5-12H2,1-4H3,(H,17,18)(H,19,20)
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| Chemical Name |
6,6'-Oxybis(2,2-dimethylhexanoic acid)
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| Synonyms |
PD72953; PD 72953; PD-72953; Gemcabene
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~330.68 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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