| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
PPAR-γ (IC50 = 18.25 μM)
MSDC-0602K targets the mitochondrial pyruvate carrier (MPC), a protein complex that transports pyruvate into the mitochondria. By modulating MPC, it alters cellular metabolism and improves insulin sensitivity. It also binds to PPARγ, but with low affinity (IC50 = 18.25 μM), which is believed to reduce the PPARγ-mediated side effects (such as weight gain and fluid retention) associated with full TZD agonists. |
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| ln Vitro |
In vitro, MSDC-0602K binds to PPARγ with an IC50 of 18.25 μM. It is characterized as a PPARγ-sparing compound, meaning it has significantly reduced PPARγ agonist activity compared to traditional TZDs. Its primary mechanism of action is through the modulation of the mitochondrial pyruvate carrier (MPC).
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| ln Vivo |
Diabetic db/db and MS-NASH mice are administered oral gavage of ezemiglitazone potassium, subcutaneous injection of ligliglutide, or a combination of zemiglitazone potassium and ligliglutide. For patients with diabetes and non-alcoholic steatohepatitis (NASH), this combination treatment may be a useful therapeutic approach.
In vivo, MSDC-0602K has been shown to improve insulin sensitivity and fatty liver disease in mice. In mouse models, it improves insulinemia and fatty liver disease, both as a monotherapy and in combination with liraglutide. It is being studied for its potential to treat fatty liver disease, including conditions with dysfunctional lipid metabolism, inflammation, and insulin resistance. |
| Enzyme Assay |
The binding of MSDC-0602K to PPARγ is assessed using standard binding assays, such as radioligand binding or surface plasmon resonance (SPR). Its effect on the mitochondrial pyruvate carrier can be assessed using cellular assays that measure pyruvate uptake or mitochondrial respiration.
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| Cell Assay |
The cellular activity of MSDC-0602K is evaluated in cell lines relevant to metabolism, such as hepatocytes or adipocytes. Its effect on insulin signaling, glucose uptake, and lipid accumulation can be measured. Its effect on mitochondrial function can be assessed using Seahorse analyzers to measure oxygen consumption rate (OCR) and extracellular acidification rate (ECAR).
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| Animal Protocol |
Five-week-old male db/db mice on C57BL/6J background and age/sex-matched db/+ control mice
30 mg/kg MSDC-0602K; 0.2 mg/kg Liraglutide (obtained from MedChemExpress) MSDC-0602K gavage daily, Liraglutide s.c. injection every other day, or combined MSDC-0602K+ Liraglutide In animal studies, MSDC-0602K is typically administered orally to rodent models of metabolic disease, such as diet-induced obesity or fatty liver models. Its effect on insulin sensitivity is assessed by glucose tolerance tests and hyperinsulinemic-euglycemic clamps. Its effect on liver steatosis is assessed by histology and measuring liver triglyceride content. |
| ADME/Pharmacokinetics |
Pharmacokinetic studies of MSDC-0602K indicate that it has properties suitable for oral administration. Its half-life and exposure are consistent with once- or twice-daily dosing. Its metabolism and excretion pathways are characteristic of small molecule drugs.
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| Toxicity/Toxicokinetics |
Toxicology data for MSDC-0602K is not provided in the available literature. As a clinical candidate, its safety profile would have been evaluated in preclinical toxicology studies.
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| References |
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| Additional Infomation |
MSDC-0602K (Azemiglitazone potassium, CAS: 1314533-27-1) is a next-generation insulin sensitizer that modulates the mitochondrial pyruvate carrier while sparing PPARγ. This unique mechanism is designed to provide the metabolic benefits of TZDs without the PPARγ-mediated side effects. It has shown promise in preclinical models of fatty liver disease and is a key compound for developing safer and more effective therapies for metabolic syndrome.
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| Molecular Formula |
C19H16KNO5S
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|---|---|
| Exact Mass |
409.04
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| Elemental Analysis |
C, 55.73; H, 3.94; K, 9.55; N, 3.42; O, 19.53; S, 7.83
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| CAS # |
1314533-27-1
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| Related CAS # |
Azemiglitazone;1133819-87-0
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| PubChem CID |
87355566
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
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| Complexity |
538
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PQCFIIIBRQVVGW-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C19H17NO5S.K/c1-24-15-4-2-3-13(10-15)16(21)11-25-14-7-5-12(6-8-14)9-17-18(22)20-19(23)26-17;/h2-8,10,17H,9,11H2,1H3,(H,20,22,23);/q;+1/p-1
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| Chemical Name |
potassium;5-[[4-[2-(3-methoxyphenyl)-2-oxoethoxy]phenyl]methyl]-1,3-thiazolidin-3-ide-2,4-dione
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| Synonyms |
MSDC 0602; MSDC0602; MSDC-0602; MSDC-0602 potassium
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: 82~250 mg/mL (200.2~610.5 mM)
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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.) |
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 |
| NCT03970031 | Not yet recruiting | Drug: MSDC-0602K Drug: Placebo |
Nonalcoholic Steatohepatitis Type2 Diabetes |
Cirius Therapeutics, Inc. | June 2022 | Phase 3 |
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