INT 131 - CAS 315224-26-1
Catalog number: 315224-26-1
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C21H12Cl4N2O3S
Molecular Weight:
511.93
COA:
Inquire
Targets:
PPAR
Description:
INT 131 is a hypoglycemic agent, displays robust glucose-lowering activity in rodent models of diabetes while exhibiting a reduced side-effects profile compared to marketed TZDs.
Purity:
≥98%
Appearance:
Solid powder
Synonyms:
AMG-131; AMG 131; AMG131; INT-131; NT-131; INT-131; T-0903131; T-1312,4-Dichloro-N-(3,5-dichloro-4-quinolin-3-yloxyphenyl)benzenesulfonamide;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
Selective PPARgamma modulator, enhancing insulin sensitivity.
Quality Standard:
Enterprise standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly.
Quantity:
Milligrams-Grams
InChIKey:
NMRWDFUZLLQSBN-UHFFFAOYSA-N
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
Canonical 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
Current Developer:
InteKrin Therapeutics
1.INT131 increases dendritic arborization and protects against Aβ toxicity by inducing mitochondrial changes in hippocampal neurons.
Godoy JA;Zolezzi JM;Inestrosa NC Biochem Biophys Res Commun. 2017 Aug 26;490(3):955-962. doi: 10.1016/j.bbrc.2017.06.146. Epub 2017 Jun 24.
In previous studies, we have demonstrated the beneficial effects of classic PPARγ agonists on neuroprotection against Aβ oligomer neurotoxicity in a double transgenic mouse model of Alzheimer' disease (AD). INT-131, a novel, non-thiazolidinedione compound that belongs to a new family of drugs, selective PPARγ modulators (SPPARMs), has provided an emerging opportunity for the treatment of type 2 diabetes mellitus and metabolic syndrome. However, its role in the central nervous system has not been studied. The aim of this study was to evaluate the putative neuroprotective role of INT131 in hippocampal neurons. We found that INT131 increased dendritic branching, promoted neuronal survival against Aβ amyloid, increased expression of PGC1-1α and modulated neuronal mitochondrial dynamics. Our results suggest that INT131, a drug that has been shown to be safe and effective in metabolic disorders, may constitute a new therapeutic alternative for AD.
2.PAR-1622 is a selective peroxisome proliferator-activated receptor gamma partial activator with preserved antidiabetic efficacy and broader safety profile for fluid retention.
Kim MK;Chae YN;Kim HS;Choi SH;Son MH;Kim SH;Kim JK;Moon HS;Park SK;Shin YA;Kim JG;Lee CH;Lim JI;Shin CY Arch Pharm Res. 2009 May;32(5):721-7. doi: 10.1007/s12272-009-1511-8. Epub 2009 May 27.
Peroxisome proliferator-activated receptor (PPAR) gamma is known to be a key regulator of insulin resistance. PAR-1622 is a novel small molecule compound synthesized in Dong-A research center. In this study, we characterized the pharmacological profiles of PAR-1622, a selective partial activator of PPARgamma. In transient transactivation assays, PAR-1622 [(S)-2-ethoxy-3(4-(5-(4-(5-(methoxymethyl)isoxazol-3-yl)phenyl)-3-methylthiophen-2-yl)methoxy)phenyl)propanoic acid] showed a partial activator against human PPARgamma with an EC(50) of 41 nM and a maximal response of 37% relative to the full agonist rosiglitazone without activating human PPARdelta. PAR-1622 was 56 folds more selective for human PPARgamma than for human PPARalpha (EC(50), 2304 nM), which means that it is a selective partial activator of PPARgamma. PAR-1622 also showed a partial activator against mouse PPARgamma with an EC(50) of 427 nM and a maximal response was 57% of that of rosiglitazone. INT-131, a selective PPARgamma partial agonist in clinical stage, also was a partial activator against human PPARgamma with an EC(50) of 83 nM and a maximal response achieved by INT-131 was 49% of that observed with full agonist rosiglitazone.
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