Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C19H18N2O4S |
| Molecular Weight | 370.422 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCC1=CC=C(N=C1)C(=O)COC2=CC=C(CC3SC(=O)NC3=O)C=C2
InChI
InChIKey=IRNJSRAGRIZIHD-UHFFFAOYSA-N
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)
Mitoglitazone (previously known as MSDC-0160 or CAY-10415) is a mTOT (mitochondrial target of thiazolidinediones) modulator that targets the mitochondrial pyruvate carrier (MPC), which is a key controller of cellular metabolism. MSDC-0160 is modulated MPC and act as insulin sensitizers without activating PPAR gamma. (Mitoglitazone exhibits very low binding affinity and activity at PPARγ). Mitoglitazone has been used in trials phase II studying the treatment of Type 2 Diabetes and Alzheimer's disease; the treatment for diabetes was discontinued. In addition, MSDC-0160 has demonstrated significant neuroprotective effects in the En1+/- mouse model of Parkinson’s disease via modulation of the mTOR-autophagy signaling cascade.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: Q9Y5U8 Gene ID: 51660.0 Gene Symbol: MPC1 Target Organism: Homo sapiens (Human) |
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Target ID: O95563 Gene ID: 25874.0 Gene Symbol: MPC2 Target Organism: Homo sapiens (Human) |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2800 ng/mL |
50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
MITOGLITAZONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
32000 ng × h/mL |
50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
MITOGLITAZONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
50000 ng × h/mL |
50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
MITOGLITAZONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
90000 ng × h/mL |
150.02 mg 1 times / day multiple, oral dose: 150.02 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
MITOGLITAZONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
12 h |
50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
MITOGLITAZONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
PubMed
| Title | Date | PubMed |
|---|---|---|
| An evaluation of MSDC-0160, a prototype mTOT modulating insulin sensitizer, in patients with mild Alzheimer's disease. | 2014 |
|
| Correlation between activation of PPARγ and resistin downregulation in a mouse adipocyte cell line by a series of thiazolidinediones. | 2013-08 |
|
| Clinical proof-of-concept study with MSDC-0160, a prototype mTOT-modulating insulin sensitizer. | 2013-04 |
|
| Novel insulin sensitizer modulates nutrient sensing pathways and maintains β-cell phenotype in human islets. | 2013 |
Patents
Sample Use Guides
Treatment of Human Islets with MSDC-0160 (MITOGLITAZONE) activates AMPK and downregulates mTOR. Human islets were cultured with 5 mM glucose and MSDC-0160 (1–50 µM) for 24 h. Phosphorylation of mTOR was significantly decreased at 20 and 50 µM MSDC-0160. This inhibition inversely correlated with increased phosphorylation of AMPK and its downstream target acetyl CoA carboxylase (ACC). Consistent with the reduction in the amount of phosphorylated mTOR, treatment with MSDC-0160 also produced a decrease in the phosphorylation of S6, a downstream indicator of the mTOR pathway. This was evident after 4 days of culture under these conditions, but occurred as early as 90 minutes into the treatment. Taken together, these data suggest that MSDC-0160 restores the insulin signaling pathway at least in part by modulating mTOR activity.
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DB11721
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ACTIVE MOIETY
