MSDC-0160

SKU: orb1226229

Description

A new generation insulin sensitizer and mitochondrial target of thiazolidinediones (mTOT) modulator that has low affinity for binding and activation of PPARγ (EC50=23.7 uM) and shows insulin-sensitizing effects in mouse models of diabetes; increases AMPK activity and reduces mTOR activity, maintains β-cell phenotype in human islets.Diabetes Phase 2 Clinical(In Vitro):MSDC 0160 (Mitoglitazone; 1-50 μM; for 24 hours) significantly decreases phosphorylation of mTOR at 20 and 50 μM.MSDC 0160 acts as insulin sensitizers without activating PPARγ.MSDC 0160 (10 μM; pretreatment 1 hour) prevents the MPP+ (10 μM)-induced loss of both tyrosine hydroxylase (TH)-immunoreactive differentiated Lund human mesencephalic (LUHMES) cells.MSDC 0160 (10 or 100 μM) prevents the loss of GFP-fluorescent dopaminergic neurons induced by MPP+ (0.75 mM) in nematodes.MSDC 0160 (10-20 μM) in conbination with IGF-1 prevents the loss of insulin content and maintains insulin secretion.MSDC 0160 (1-50 μM) treatment maintains human β-cell phenotype.(In Vivo):MSDC 0160 (Mitoglitazone; 30 mg/kg; oral gavage; daily; for 7 days) improves locomotor behavior, increases survival of nigral dopaminergic neurons, boosts striatal dopamine levels, and reduces neuroinflammation in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated mice.

Key Properties

• CAS Number: 146062-49-9
• MW: 370.4222
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₈N₂O₄S
• SMILES: O=C(N1)SC(CC2=CC=C(OCC(C3=NC=C(CC)C=C3)=O)C=C2)C1=O
• Target: Insulin Receptor
• Solubility: DMSO: ≥ 30 mg/mL

Bioactivity

• In Vivo:
  Animal model: Ten-to 12-week-old male C57BL/6J mice weighing 24 to 28 g. Dosage: 30 mg/kg. Administration: Oral gavage; daily; for 7 days. Result: Improved locomotor behavior, increased survival of nigral dopaminergic neurons, boosted striatal dopamine levels, and reduced neuroinflammation.
• In Vitro:
  Western blot analysis. Cell line: Human islets. Concentration: 1, 10, 20, 50 μM. Incubation time: For 24 hours. Result: Significantly decreased Phosphorylation of mTOR at 20 and 50 μM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PNU-91325 | Mitoglitazone

Quick Database Links

Gene Symbol

Insulin Receptor