INT-131

Product NameINT-131
CAS315224-26-1
MFC21H12Cl4N2O3S
MW514.21
EINECS
MOL File315224-26-1.mol

Chemical Properties

Boiling point	611.8±65.0 °C(Predicted)
Density	1.585±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO : 250 mg/mL (486.18 mM; Need ultrasonic)
pka	5.30±0.10(Predicted)
form	Solid
color	White to light yellow
InChI	1S/C21H12Cl4N2O3S/c22-13-5-6-20(16(23)8-13)31(28,29)27-14-9-17(24)21(18(25)10-14)30-15-7-12-3-1-2-4-19(12)26-11-15/h1-11,27H
InChIKey	NMRWDFUZLLQSBN-UHFFFAOYSA-N
SMILES	[S](=O)(=O)(Nc2cc(c(c(c2)Cl)Oc3cnc4c(c3)cccc4)Cl)c1c(cc(cc1)Cl)Cl

Safety Information

Storage Class

11 - Combustible Solids

Usage And Synthesis

Uses

AMG131 (INT131) is a potent non-thiazolidinedione (TZD) selective peroxisome proliferator-activated receptor γ modulator (SPPARM). AMG131 binds to PPARγ within the same binding pocket as the TZDs, but occupies a unique space in the pocket and contacts the receptor at distinct points from the TZDs. AMG131 is promising for research of type-2 diabetes mellitus[1][2][3].

Biological Activity

INT131 is a brain penetrant, non-thiazolidinedione, highly potent and selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator (SPPARM) th at displays anti-diabetic activities. INT131 is a partial, rather than a full agonist of PPARγ, and in clinical trials has shown increased glucose tolerance without the weight gain and cardiovascular side effects seen with some of the full agonist.

in vivo

AMG131 (INT131; 80 mg/kg; 14-day oral treatment) increases in glucose tolerance in Zucker (fa/fa) rats following^[2]

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.

IC 50

PPARγ

storage

Store at -20°C

References

[1] Linda S Higgins,et al. The Development of INT131 as a Selective PPARgamma Modulator: Approach to a Safer Insulin Sensitizer. PPAR Res. 2008;2008:936906. DOI:10.1155/2008/936906
[2] Alykhan Motani, et al. INT131: a selective modulator of PPAR gamma. J Mol Biol. 2009 Mar 13;386(5):1301-11. DOI:10.1016/j.jmb.2009.01.025
[3] Higgins LS, et al. The Development of INT131 as a Selective PPARgamma Modulator: Approach to a Safer Insulin Sensitizer. PPAR Res. 2008;2008:936906. DOI:10.1155/2008/936906

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