[CAS NO. 315224-26-1] AMG131

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PRODUCTS SPECIFICATIONS [315224-26-1]

Catalog

AS983544

Brand

Arctom Scientific

CAS

315224-26-1

DESCRIPTION [315224-26-1]

Overview

MDL	MFCD13152369
Molecular Weight	514.21
Molecular Formula	C21H12Cl4N2O3S
SMILES	O=S(C1=CC=C(Cl)C=C1Cl)(NC2=CC(Cl)=C(OC3=CC4=CC=CC=C4N=C3)C(Cl)=C2)=O

For research use only. We do not sell to patients.

Summary

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) ^[1] ^[2] .

IC50 & Target

PPARγ

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 ^[1] .

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 following ^[2]

MCE 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 weeks ^[2]
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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02638038	InteKrin Therapeutics, Inc.	Multiple Sclerosis, Relapsing Remitting	February 2015	Phase 2
NCT00631007	InteKrin Therapeutics, Inc.	Type 2 Diabetes Mellitus	February 2008	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL ( 486.18 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9447 mL	9.7237 mL	19.4473 mL
5 mM	0.3889 mL	1.9447 mL	3.8895 mL
10 mM	0.1945 mL	0.9724 mL	1.9447 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.05 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.05 mM); Clear solution

* All of the co-solvents are available by MCE.