| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Aramchol targets stearoyl-CoA desaturase 1 (SCD1), the rate-limiting enzyme in the synthesis of monounsaturated fatty acids. By inhibiting SCD1 expression in hepatocytes and hepatic stellate cells, aramchol reduces fatty acid synthesis and lipid accumulation in the liver. This leads to a decrease in liver fat content and improvement in liver function. Aramchol is a cholesterol solubilizer that prevents gallstone formation. Its dual mechanism of action makes it a promising therapeutic for NASH and NAFLD.
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| ln Vitro |
In vitro, aramchol inhibits SCD1 expression in hepatocytes and hepatic stellate cells. As a cholesterol solubilizer, it prevents gallstone formation. It is an orally active novel fatty acid bile acid coupling agent. In cell-based assays, aramchol can reduce lipid accumulation in hepatocytes and decrease the expression of SCD1. The compound's effects on cholesterol solubility can be assessed in cell-free systems.
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| ln Vivo |
In vivo, aramchol has been shown to reduce liver fat content in patients with NAFLD. It prevents gallstone formation in inbred mice. It has been used in clinical trials to study the treatment of diseases such as HIV, gallstones, fatty liver, metabolic syndrome, and NASH. The compound is orally active, indicating good oral bioavailability. Its effects on liver fat, inflammation, and fibrosis have been evaluated in clinical studies.
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| Enzyme Assay |
Non-cellular in vitro assays for aramchol involve measuring its inhibition of SCD1 enzyme activity. A typical protocol uses a cell-free system with microsomal fractions containing SCD1. The enzyme is incubated with its substrate, stearoyl-CoA, and varying concentrations of aramchol. The production of oleoyl-CoA is measured by HPLC or by a radiometric assay. The IC50 for SCD1 inhibition is determined. Alternatively, cholesterol solubilization assays can be performed to assess the compound's ability to solubilize cholesterol in bile acid solutions.
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| Cell Assay |
Cellular assays for aramchol are performed using hepatocyte cell lines such as HepG2 or primary human hepatocytes. Cells are treated with aramchol at various concentrations for 24-48 hours. SCD1 expression is measured by RT-PCR or Western blotting. Lipid accumulation is assessed by Oil Red O staining or by measuring triglyceride content. The inhibition of SCD1 expression and reduction of lipid accumulation are quantified. Cell viability is measured using an MTT assay.
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| Animal Protocol |
In vivo animal studies for aramchol are conducted in mouse models of gallstone disease or NAFLD/NASH. Mice are fed a lithogenic diet to induce gallstone formation, and aramchol is administered orally to assess its ability to prevent gallstones. In NAFLD/NASH models, mice are fed a high-fat diet, and aramchol is administered orally. Liver fat content is measured by histology or biochemical assay. Liver enzymes and markers of inflammation and fibrosis are measured in blood and liver tissue.
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| ADME/Pharmacokinetics |
Aramchol has a molecular formula of C44H79NO5 and a molecular weight of 702.10. It is an orally active compound. It has a density of 1.05±0.1 g/cm3 (20 ºC) and is practically insoluble in water (6.2e-7 g/L at 25 ºC). For in vivo studies, it can be formulated in standard vehicles for oral administration. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability have been reported from clinical trials, but are not detailed in the available literature.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for aramchol have been reported from clinical trials. As a clinical-stage compound, it has been evaluated for safety in humans. Common side effects may include gastrointestinal disturbances. However, specific toxicity data are not detailed in the available literature. Aramchol is not a clinically approved drug but has been studied in clinical trials for NASH and NAFLD.
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| References | |
| Additional Infomation |
Aramchol has been used in clinical trials to study the treatment of diseases such as HIV, gallstones, fatty liver, metabolic syndrome, and non-alcoholic steatohepatitis.
Aramchol (C20-FABAC) is an orally active novel fatty acid bile acid coupling agent and an inhibitor of SCD1. It is a conjugate of cholic acid and arachidic acid. Aramchol is a cholesterol solubilizer that prevents gallstone formation in inbred mice. It reduces liver fat content in patients with NAFLD. Aramchol has been used in clinical trials to study the treatment of diseases such as HIV, gallstones, fatty liver, metabolic syndrome, and NASH. Aramchol is not a clinically approved drug but has reached clinical trials for NASH and NAFLD. |
| Molecular Formula |
C44H79NO5
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|---|---|
| Molecular Weight |
702.101774454117
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| Exact Mass |
701.595
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| CAS # |
246529-22-6
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| PubChem CID |
18738120
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
806.0±65.0 °C at 760 mmHg
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| Flash Point |
441.3±34.3 °C
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| Vapour Pressure |
0.0±6.5 mmHg at 25°C
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| Index of Refraction |
1.529
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| LogP |
11.85
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
23
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| Heavy Atom Count |
50
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| Complexity |
1020
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| Defined Atom Stereocenter Count |
11
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| SMILES |
C(CC[C@@H](C)[C@H]1CC[C@@H]2[C@@]1([C@H](C[C@H]1[C@H]2[C@H](O)C[C@H]2[C@@]1(CC[C@@H](C2)NC(CCCCCCCCCCCCCCCCCCC)=O)C)O)C)(=O)O
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| InChi Key |
SHKXZIQNFMOPBS-OOMQYRRCSA-N
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| InChi Code |
InChI=1S/C44H79NO5/c1-5-6-7-8-9-10-11-12-13-14-15-16-17-18-19-20-21-22-40(48)45-34-27-28-43(3)33(29-34)30-38(46)42-36-25-24-35(32(2)23-26-41(49)50)44(36,4)39(47)31-37(42)43/h32-39,42,46-47H,5-31H2,1-4H3,(H,45,48)(H,49,50)/t32-,33+,34+,35-,36+,37+,38-,39+,42+,43+,44-/m1/s1
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| Chemical Name |
(R)-4-((3S,5S,7R,8R,9S,10S,12S,13R,14S,17R)-7,12-dihydroxy-3-icosanamido-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentanoic
acid
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| Synonyms |
C20-FABACC20FABACC20FABACArachidyl amido cholanoic acid
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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 : ~25 mg/mL (~35.61 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.96 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 20.8 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: ≥ 2.08 mg/mL (2.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4243 mL | 7.1215 mL | 14.2430 mL | |
| 5 mM | 0.2849 mL | 1.4243 mL | 2.8486 mL | |
| 10 mM | 0.1424 mL | 0.7121 mL | 1.4243 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NOT YET RECRUITING | NOT YET RECRUITING | Drug: Aramchol meglumine Drug: Aramchol free acid |
Healthy | Galmed Pharmaceuticals Ltd | 2024-10 | Phase 1 |
| NCT01094158 | COMPLETED | Drug: Aramchol Drug: Aramchol Drug: Placebo |
Metabolic Syndrome Non-Alcoholic Fatty Liver Disease Nonalcoholic Steatohepatitis |
Galmed Medical Reserch | 2010-11 | Phase 2 |
| NCT00776841 | COMPLETED | Drug: Aramchol Drug: Aramchol Drug: Aramchol |
Healthy | Galmed Medical Reserch | 2008-09 | Phase 1 |
| NCT05874336 | COMPLETED | Drug: Aramchol | NASH | Galmed Pharmaceuticals Ltd | 2020-06-17 | Phase 1 |
| NCT03774173 | COMPLETED | Drug: Aramchol | Healthy | Galmed Pharmaceuticals Ltd | 2018-12-08 | Phase 1 |
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