MSDC-0160

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

新一代胰岛素增敏剂和噻唑烷二酮类线粒体靶标 (mTOT) 调节剂，对 PPARγ 的结合和激活具有低亲和力 (EC50=23.7 uM)。

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.

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.

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.

PNU-91325 | Mitoglitazone

Tyrosine Kinase

Insulin Receptor

mTOT

Metabolic Disease

Diabetes

146062-49-9

370.4222

C19H18N2O4S

>98% (HPLC)

DMSO: ≥ 30 mg/mL

O=C(N1)SC(CC2=CC=C(OCC(C3=NC=C(CC)C=C3)=O)C=C2)C1=O

2,4-Thiazolidinedione, 5-[[4-[2-(5-ethyl-2-pyridinyl)-2-oxoethoxy]phenyl]methyl]-

(-20℃)

With Ice Pack

≥ 2 years