AMG131 - Moligand™,10mM in DMSO , Peroxisome proliferator-activated receptor gamma modulator, CAS No.315224-26-1, Peroxisome proliferator-activated receptor gamma modulator

CAS: 315224-26-1 Cat. No.: A656660 Molecular Weight: 514.21 PubChem CID: 10229498

GRADE & PURITY Moligand™, 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a K i of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM)

In Vitro

AMG131 (INT131) binds to PPARγ and displaces Rosiglitazone with a K i 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 K i for PPARγ. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AMG131 (INT131; 80 mg/kg; 14-day oral treatment) increases in glucose tolerance in Zucker (fa/fa) rats followingMCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Zucker fatty (fa/fa) rats ages 7-8 weeksDosage: 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.

IC50& Target:PPARγ

Specifications

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a K i of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM).

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

MODULATOR

Mechanism of action

Peroxisome proliferator-activated receptor gamma modulator

Product Properties

• ALogP: 6.8

Names and Identifiers

• Isomeric SMILES: 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
• Alternate CAS: 315224-26-1
• PubChem CID: 10229498
• MeSH Entry Terms: AMG 131;AMG-131;AMG131;INT 131;INT-131;INT131;T 0903131;T 131 cpd;T-0903131;T-131 cpd;T0903131;T131 cpd
• Molecular Weight: 514.21

Associated Targets(Human)

PPARG Tclin Peroxisome proliferator-activated receptor gamma (5 Activities)

Discover Target: PPARG

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)