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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
MEDICA16 targets ATP-citrate lyase, an enzyme involved in lipogenesis, and acts as an agonist at the free fatty acid 1 (FFA1/GPR40) receptor. By inhibiting ATP-citrate lyase, it reduces the synthesis of fatty acids and cholesterol. Activation of GPR40 enhances glucose-stimulated insulin secretion. It also acts as a partial agonist for GPR120. Its mechanism of action contributes to its hypolipidemic and antidiabetogenic properties.
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| ln Vitro |
In vitro, MEDICA16 inhibits ATP-citrate lyase activity, leading to a reduction in intracellular triacylglycerol levels in muscle cells. It activates GPR40-mediated signaling pathways, which can be measured by downstream effects such as calcium mobilization. Its potency and selectivity for GPR40 over GPR120 have been characterized in cell-based assays.
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| ln Vivo |
In vivo, MEDICA16 functions to blunt the development of insulin resistance in the JCR:LA-cp rat model. It acts as a potent triacylglycerol-lowering agent, reducing serum lipid levels. It increases insulin sensitivity in rodents, making it a promising agent for research in metabolic diseases. Its effects are dose-dependent and related to its dual mechanism as an ATP-citrate lyase inhibitor and GPR40 agonist.
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| Enzyme Assay |
In vitro enzyme/receptor binding studies for MEDICA16 involve assays for ATP-citrate lyase inhibition and GPR40 receptor binding. ATP-citrate lyase activity is measured by monitoring the conversion of citrate and CoA to acetyl-CoA and oxaloacetate. GPR40 binding affinity is assessed using radioligand binding assays with membrane preparations from cells expressing the receptor. Functional assays measure GPR40-mediated calcium mobilization or signaling pathways.
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| Cell Assay |
In vitro cellular assays for MEDICA16 involve culturing cells such as muscle cells or pancreatic beta-cells in the presence of serial dilutions of the compound. Intracellular triacylglycerol content is measured to assess lipogenesis inhibition. GPR40 activation is assessed by measuring intracellular calcium mobilization or insulin secretion. Cell viability is assessed using standard assays to determine the compound's safety profile.
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| Animal Protocol |
In vivo animal studies for MEDICA16 are conducted in rodent models of insulin resistance and hyperlipidemia, such as the JCR:LA-cp rat. Animals are treated with MEDICA16 via oral administration. Endpoints include measurements of blood glucose, insulin levels, lipid profiles, and insulin sensitivity. Standard protocols include dose-response assessment and comparison to vehicle or reference treatments.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MEDICA16 include good solubility in DMSO (69 mg/mL) and it is insoluble in water and ethanol. It has a molecular weight of 342.51. For in vivo studies, it can be formulated as a homogeneous suspension in CMC-Na. Detailed pharmacokinetic parameters such as half-life and bioavailability are available from preclinical studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity data for MEDICA16 are limited, as it is a research compound. In animal studies, it is generally well-tolerated at efficacious doses. Standard toxicology parameters such as body weight, organ weight, and histopathology are monitored in long-term studies. Further toxicity studies are required for clinical development. It is intended for research use only and is not approved for human therapeutic use.
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| References |
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| Additional Infomation |
MEDICA 16 is an α,ω-dicarboxylic acid, namely hexadecanoic acid, with methyl groups at positions 3 and 14. It is a free fatty acid 1 (FFA1/GPR40) receptor agonist and an ATP citrate lyase inhibitor, possessing lipid-lowering and antidiabetic effects. It can be used as a lipid-lowering drug, an EC 6.4.1.2 (acetyl-CoA carboxylase) inhibitor, an EC 2.3.3.8 (ATP citrate synthase) inhibitor, a G protein-coupled receptor agonist, and a hypoglycemic agent.
MEDICA16 is a valuable research tool for studying lipid metabolism, insulin resistance, and the role of GPR40 in metabolic diseases. It is also known as a free fatty acid 1 (FFA1/GPR40) receptor agonist. It is commercially available for research purposes from various chemical suppliers. It is not approved for clinical use and has no established therapeutic indications. Its dual mechanism makes it a unique compound for studying the interplay between lipid synthesis and insulin sensitivity. |
| Molecular Formula |
C20H36NA2O4
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|---|---|
| Molecular Weight |
386.4835
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| Exact Mass |
342.277
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| CAS # |
87272-20-6
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| PubChem CID |
121871
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
485.9±18.0 °C at 760 mmHg
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| Melting Point |
154-159ºC
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| Flash Point |
261.8±17.7 °C
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| Vapour Pressure |
0.0±2.6 mmHg at 25°C
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| Index of Refraction |
1.474
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| LogP |
6.44
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
24
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| Complexity |
336
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HYSMCRNFENOHJH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H38O4/c1-19(2,15-17(21)22)13-11-9-7-5-6-8-10-12-14-20(3,4)16-18(23)24/h5-16H2,1-4H3,(H,21,22)(H,23,24)
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| Chemical Name |
3,3,14,14-tetramethylhexadecanedioic acid
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| Synonyms |
MEDICA16; MEDICA-16; MEDICA 16
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5875 mL | 12.9373 mL | 25.8746 mL | |
| 5 mM | 0.5175 mL | 2.5875 mL | 5.1749 mL | |
| 10 mM | 0.2587 mL | 1.2937 mL | 2.5875 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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