INT-131

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

INT-131 是一种新型非噻唑烷二酮 (TZD)、选择性过氧化物酶体增殖物激活受体 (PPAR) γ 调节剂。

INT-131, is a novel, non-thiazolidinedione (TZD), selective peroxisome proliferator-activated receptor (PPAR)gamma modulator, which can be used for the treatment of type 2 diabetes mellitus (non-insulin dependent diabetes)(In Vitro):AMG131 (INT131) binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM, demonstrating ~20-fold higher affinity than either Rosiglitazone or Pioglitazone, and with greater than 1000-fold selectivity for PPARγ over PPARα, PPARδ, or a set of other nuclear receptors. AMG131 is highly selective for PPARγ, with no binding to PPARα or δ at 10 μM, 1000 fold over the Ki for PPARγ.(In Vivo):AMG131 (INT131; 80 mg/kg; 14-day oral treatment) increases in glucose tolerance in Zucker (fa/fa) rats following.

AMG131 (INT131) binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM, demonstrating ~20-fold higher affinity than either Rosiglitazone or Pioglitazone, and with greater than 1000-fold selectivity for PPARγ over PPARα, PPARδ, or a set of other nuclear receptors. AMG131 is highly selective for PPARγ, with no binding to PPARα or δ at 10 μM, 1000 fold over the Ki for PPARγ.

AMG131 (INT131; 80 mg/kg; 14-day oral treatment) increases in glucose tolerance in Zucker (fa/fa) rats following Animal Model:Male Zucker fatty (fa/fa) rats ages 7-8 weeks Dosage:80 mg/kg Administration: Administered once daily by oral gavage for 14 days Result:Exhibited maximal efficacy comparable to that of Rosiglitazone with respect to plasma glucose clearance in an oral glucose tolerance test. Reduced baseline insulin levels, similar to Rosiglitazone, could improve insulin sensitivity in treated animals.

AMG-131 | CHS 131

Metabolic Enzyme/Protease

PPAR

PPARγ

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315224-26-1

514.21

C21H12Cl4N2O3S

>98% (HPLC)

DMSO:10 mM

C1=CC=C2C(=C1)C=C(C=N2)OC3=C(C=C(C=C3Cl)NS(=O)(=O)C4=C(C=C(C=C4)Cl)Cl)Cl

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(-20℃)

With Ice Pack

≥ 2 years