Indeglitazar - CAS 835619-41-5
Catalog number: 835619-41-5
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C19H19NO6S
Molecular Weight:
389.43
COA:
Inquire
Targets:
PPAR
Description:
Indeglitazar is a peroxisome proliferator-activated receptor (PPAR) pan-agonist. Phase II clinical trials for Type 2 diabetes mellitus was discontinued.
Purity:
98%
Appearance:
Powder
Synonyms:
PLX-204; PLX204; PLX 204; PPM-204; PPM204; PPM 204; Indeglitazar; 3-(5-Methoxy-1-((4-methoxyphenyl)sulfonyl)-1H-indol-3-yl)propanoic acid
Solubility:
Soluble in DMSO
Storage:
-20℃ Freezer
MSDS:
Inquire
Application:
Type 2 diabetes mellitus
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
YMPALHOKRBVHOJ-UHFFFAOYSA-N
InChI:
1S/C19H19NO6S/c1-25-14-4-7-16(8-5-14)27(23,24)20-12-13(3-10-19(21)22)17-11-15(26-2)6-9-18(17)20/h4-9,11-12H,3,10H2,1-2H3,(H,21,22)
Canonical SMILES:
O=C(O)CCC1=CN(S(=O)(C2=CC=C(OC)C=C2)=O)C3=C1C=C(OC)C=C3
Current Developer:
Originator Plexxikon
1.Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent.
Artis DR;Lin JJ;Zhang C;Wang W;Mehra U;Perreault M;Erbe D;Krupka HI;England BP;Arnold J;Plotnikov AN;Marimuthu A;Nguyen H;Will S;Signaevsky M;Kral J;Cantwell J;Settachatgull C;Yan DS;Fong D;Oh A;Shi S;Womack P;Powell B;Habets G;West BL;Zhang KY;Milburn MV;Vlasuk GP;Hirth KP;Nolop K;Bollag G;Ibrahim PN;Tobin JF Proc Natl Acad Sci U S A. 2009 Jan 6;106(1):262-7. doi: 10.1073/pnas.0811325106. Epub 2008 Dec 30.
In a search for more effective anti-diabetic treatment, we used a process coupling low-affinity biochemical screening with high-throughput co-crystallography in the design of a series of compounds that selectively modulate the activities of all three peroxisome proliferator-activated receptors (PPARs), PPARalpha, PPARgamma, and PPARdelta. Transcriptional transactivation assays were used to select compounds from this chemical series with a bias toward partial agonism toward PPARgamma, to circumvent the clinically observed side effects of full PPARgamma agonists. Co-crystallographic characterization of the lead molecule, indeglitazar, in complex with each of the 3 PPARs revealed the structural basis for its PPAR pan-activity and its partial agonistic response toward PPARgamma. Compared with full PPARgamma-agonists, indeglitazar is less potent in promoting adipocyte differentiation and only partially effective in stimulating adiponectin gene expression. Evaluation of the compound in vivo confirmed the reduced adiponectin response in animal models of obesity and diabetes while revealing strong beneficial effects on glucose, triglycerides, cholesterol, body weight, and other metabolic parameters.
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CAS 835619-41-5 Indeglitazar

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