ChemicalBook CAS DataBase List 315224-26-1

315224-26-1

Name	INT-131
CAS	315224-26-1
Molecular Formula	C21H12Cl4N2O3S
MDL Number	MFCD13152369
Molecular Weight	514.21
MOL File	315224-26-1.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)
form	Solid
pka	5.30±0.10(Predicted)
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 Data

Storage Class

11 - Combustible Solids

Hazard Information

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

Spectrum Detail

Supplier

Shanghai Boyle Chemical Co., Ltd.

Telephone

Websitehttp://www.boylechem.com

Struchem Co., Ltd.

Telephone0512-63009836 18994340901

Websitehttp://www.beidapharma.com

Shanghai EFE Biological Technology Co., Ltd.

Telephone021-65675885 18964387627

Websitehttp://www.efebio.com

Shanghai YuanYe Biotechnology Co., Ltd.

Telephone 13636370518

Websitehttps://www.shyuanye.com

ShangHai Biochempartner Co.,Ltd

Telephone177-54423994 17754423994

Websitehttps://www.biochempartner.com

Shanghai Chaolan Chemical Technology Center

TelephoneQQ：65489617 13301690235

Websitehttp://www.atkchemical.com/

Amadis Chemical Company Limited

Telephone571-89925085

Websitehttp://www.amadischem.com

Shanghai Biopharmaleader Co., Ltd.

Telephone+86 18721201413

Websitehttp://www.biopharmaleader.com

Beijing Minruida Technology Co., Ltd.

Telephone010-82387566

Websitehttp://www.mreda.com.cn/

Nextpeptide Inc

Telephone+86-0571-81612335 +8613336028439

Websitehttp://www.nextpeptide.com/

Changzhou Xuanye Technology Co., Ltd

Telephone 15195022192;

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList152306/0_EN.htm

Shanghai Luofa Biochemical Technology Co., Ltd.

Telephone021-51111890 15317326293

Websitehttps://www.molnova.cn/

Shanghai Xiushi Biomedical Co., LTD

Telephone15002184385 15021598081 15002184385

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList1986421/0_EN.htm

Hangzhou Taorui Biotechnology Co., Ltd

TelephoneQQ1259737804 15268198094

Websitehttp://www.torreybio.com/

Jinan Jiuli Biotechnology Co. , Ltd.

Telephone 15865264761

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList89365/0_EN.htm

Bide Pharmatech Ltd.

Telephone400-1647117 13681763483

Websitehttps://www.bidepharm.com/

InvivoChem

Telephone 13549236410

Websitehttps://www.invivochem.cn/

Beijing Biocreative Technology Co., Ltd.

Telephone 15522676233

Websitehttp://www.bestbaiao.com/

1of4

Related Products

Send Inquriy