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| 10mg |
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| 25mg |
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Purity: ≥98%
Mitoglitazone (MSDC-0160; CAY10415), a thiazolidinedione analog,is the prototypical mTOT(mitochondrial target of thiazolidinediones)-modulating insulin sensitizer being investigated to treat diabetes and Alzheimer's disease. It is an insulin sensitizer free of side effects that are dependent on the peroxisome proliferator-activated receptor-γ (PPAR-γ). Insulin content is preserved and the resistance of the insulin-signaling pathway is decreased when islets are co-incubated with MSDC-0160 and IGF-1. Significantly reducing the loss of insulin content is also prevented by MSDC-0160 at 50μM. In addition, MSDC-0160 treatment results in AMPK phosphorylation being increased while mTOR phosphorylation is decreased. Furthermore, it is discovered that MSDC-0160 exhibits pro-survival effects in human islets by raising the expression of apoptosis-related genes like bcl2 and decreasing the amount of cleaved caspase-3.
| Targets |
mTOT
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|---|---|
| ln Vitro |
MSDC-0160 restores IGF-1-induced Akt and GSK-3 phosphorylation and lessens resistance in the insulin/IGF-1 signaling pathway. When combined with IGF-1 and 8 mM glucose, MSDC-0160 elevates the expression of insulin, pdx1, nkx6.1, and nkx2.2 genes specific to β-cells and preserves insulin levels without affecting glucose-stimulated insulin secretion. Additionally, MSDC-0160 decreases the expression of apoptosis markers and increases human β-cell differentiation.[1]
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| ln Vivo |
MSDC-0160 (100 mg/kg p.o.) improves insulin sensitivity by causing a significant drop in the product of circulating insulin and glucose in diabetic KKAy mice.
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| Enzyme Assay |
Even at 50μM, MSDC-0160 considerably reduces the loss of insulin content. Furthermore, treatment of MSDC-0160 decreases mTOR phosphorylation while increasing AMPK phosphorylation. Additionally, MSDC-0160 is discovered to exhibit pro-survival effects in human islets by upregulating the expression of genes linked to apoptosis, such as bcl2, and lowering the quantity of cleaved caspase-3.
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| Cell Assay |
In human β-cells, MSDC-0160 inhibits nuclear translocation by localizing β-catenin on the cytoplasm or cell membrane.
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| Animal Protocol |
Ten- to 12-week-old male C57BL/6J mice weighing 24 to 28 g
30 mg/kg Oral gavage; daily; for 7 days |
| References |
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| Molecular Formula |
C19H18N2O4S
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|---|---|
| Molecular Weight |
370.4222
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| Exact Mass |
370.10
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| Elemental Analysis |
C, 61.61; H, 4.90; N, 7.56; O, 17.28; S, 8.65
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| CAS # |
146062-49-9
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| Related CAS # |
1628078-14-7 (R-isomer);146062-49-9 (racemic);1628078-13-6 (S-isomer);
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| Appearance |
Solid powder
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| SMILES |
CCC1=CN=C(C=C1)C(=O)COC2=CC=C(C=C2)CC3C(=O)NC(=O)S3
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| InChi Key |
IRNJSRAGRIZIHD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H18N2O4S/c1-2-12-5-8-15(20-10-12)16(22)11-25-14-6-3-13(4-7-14)9-17-18(23)21-19(24)26-17/h3-8,10,17H,2,9,11H2,1H3,(H,21,23,24)
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| Chemical Name |
5-[[4-[2-(5-ethylpyridin-2-yl)-2-oxoethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione
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| Synonyms |
Mitoglitazone; CAY10415; MSDC 0160; CAY 10415; MSDC-0160;CAY-10415; CAY 10415; CAY-10415; MSDC0160; CAY10415
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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: <1 mg/mL
Water: <1 mg/mL Ethanol: <1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.75 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 (6.75 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 (6.75 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 | 2.6996 mL | 13.4982 mL | 26.9964 mL | |
| 5 mM | 0.5399 mL | 2.6996 mL | 5.3993 mL | |
| 10 mM | 0.2700 mL | 1.3498 mL | 2.6996 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 |
| NCT01374438 | Completed | Drug: MSDC-0160 Drug: Placebo |
Alzheimer's Disease | Metabolic Solutions Development Company |
July 2011 | Phase 2 |
| NCT00760578 | Completed | Drug: MSDC-0160 90 mg Drug: MSDC-0160 220 mg |
Type 2 Diabetes Mellitus | Metabolic Solutions Development Company |
September 2008 | Phase 2 |
| NCT01103414 | Completed | Drug: Mitoglitazone Drug: Pioglitazone |
Type 2 Diabetes | Metabolic Solutions Development Company |
September 2010 | Phase 2 |
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