| Size | Price | Stock | Qty |
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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 |
MK-1903 targets hydroxycarboxylic acid receptor 2 (HCA2, GPR109A), a G protein-coupled receptor that regulates lipolysis. Activation of HCA2 by MK-1903 inhibits adenylyl cyclase, reducing cAMP levels and thereby lowering free fatty acid release from adipose tissue. This mechanism underlies its potential for treating dyslipidemia and metabolic disorders.
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|---|---|
| ln Vitro |
In vitro, MK-1903 acts as a full agonist of HCA2, reducing forskolin-induced cAMP production in CHO cells expressing the human receptor with an EC50 of 12.9 nM. Its potency and selectivity have been confirmed in various in vitro assays.
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| ln Vivo |
In vivo, MK-1903 lowers free fatty acids in humans. Its efficacy in reducing lipid levels supports its potential for treating obesity and related metabolic disorders.
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| Enzyme Assay |
The in vitro receptor binding and functional assay for MK-1903 involves measuring its ability to activate HCA2 in cells expressing the receptor. The reduction in forskolin-induced cAMP production is measured using a homogenous time-resolved fluorescence (HTRF) assay. The EC50 is determined from dose-response curves.
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| Cell Assay |
Cellular assays for MK-1903 involve treating CHO cells expressing human HCA2 with the compound and measuring cAMP levels. The inhibition of cAMP production confirms its agonist activity.
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| Animal Protocol |
In vivo efficacy of MK-1903 is evaluated in human studies, where its effect on free fatty acid levels is measured.
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| ADME/Pharmacokinetics |
MK-1903 has a molecular weight of 164.16 g/mol and a molecular formula of C8H8N2O2.
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| Toxicity/Toxicokinetics |
The toxicity profile of MK-1903 is limited. As an investigational compound, comprehensive toxicological evaluations have been conducted in clinical studies.
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| References | |
| Additional Infomation |
MK-1903 is an investigational compound that has been studied for the treatment of obesity and dyslipidemia. It has not received regulatory approval. Its mechanism involves agonism of HCA2.
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| Molecular Formula |
C8H8N2O2
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|---|---|
| Molecular Weight |
164.16
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| Exact Mass |
164.058
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| CAS # |
1268882-43-4
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| PubChem CID |
49763030
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
438.1±45.0 °C at 760 mmHg
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| Flash Point |
218.7±28.7 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.732
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| LogP |
0.77
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
12
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| Complexity |
243
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1[C@H]2[C@@H]1C3=C(C2)C(=NN3)C(=O)O
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| InChi Key |
CUTZNERBKDMLAP-QWWZWVQMSA-N
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| InChi Code |
InChI=1S/C8H8N2O2/c11-8(12)7-5-2-3-1-4(3)6(5)9-10-7/h3-4H,1-2H2,(H,9,10)(H,11,12)/t3-,4-/m1/s1
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| Chemical Name |
(2R,4R)-8,9-diazatricyclo[4.3.0.02,4]nona-1(6),7-diene-7-carboxylic acid
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| Synonyms |
MK-1903; MK1903; MK 1903
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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 : ~125 mg/mL (~761.45 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (12.67 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 (12.67 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 20.8 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: ≥ 2.08 mg/mL (12.67 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 | 6.0916 mL | 30.4581 mL | 60.9162 mL | |
| 5 mM | 1.2183 mL | 6.0916 mL | 12.1832 mL | |
| 10 mM | 0.6092 mL | 3.0458 mL | 6.0916 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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