Synonym
PLX-204; PLX204; PLX 204; PPM-204; PPM204; PPM 204; Indeglitazar
IUPAC/Chemical Name
3-(5-Methoxy-1-((4-methoxyphenyl)sulfonyl)-1H-indol-3-yl)propanoic acid
InChi Key
YMPALHOKRBVHOJ-UHFFFAOYSA-N
InChi Code
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)
SMILES Code
O=C(O)CCC1=CN(S(=O)(C2=CC=C(OC)C=C2)=O)C3=C1C=C(OC)C=C3
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
Indeglitazar (PPM 204) is an orally available PPAR pan-agonist for all three PPARα, PPARδ and PPARγ.
In vitro activity:
In an assay of preadipocyte differentiation, measuring in part functional insulin sensitization capability of the cells, indeglitazar showed an EC50 of 0.32 μM compared with rosiglitazone, which showed an EC50 of 0.013 μM, although the maximal response obtained from the 2 compounds was comparable (Fig. 2D).
Reference: Proc Natl Acad Sci U S A. 2009 Jan 6;106(1):262-7. https://pubmed.ncbi.nlm.nih.gov/19116277/
In vivo activity:
Indeglitazar significantly decreased glucose, insulin, triglycerides, and free fatty acid levels (Table 3). These effects were comparable to pioglitazone on reducing glucose levels, triglycerides, and free fatty acids, although a significantly greater reduction of insulin levels were observed. As expected, pioglitazone increased adiponectin levels 3.5-fold, whereas indeglitazar raised adiponectin levels only 1.9-fold (Fig. 2F and Table 3). These data are consistent with the partial agonism observed in cell-based studies and also suggest that the insulin sensitizing activities of indeglitazar are at least partially independent of adiponectin.
Reference: Proc Natl Acad Sci U S A. 2009 Jan 6;106(1):262-7. https://pubmed.ncbi.nlm.nih.gov/19116277/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMSO |
100.0 |
256.79 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
389.42
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. 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. Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent. Proc Natl Acad Sci U S A. 2009 Jan 6;106(1):262-7. doi: 10.1073/pnas.0811325106. Epub 2008 Dec 30. PMID: 19116277; PMCID: PMC2629228.
In vitro protocol:
1. 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. Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent. Proc Natl Acad Sci U S A. 2009 Jan 6;106(1):262-7. doi: 10.1073/pnas.0811325106. Epub 2008 Dec 30. PMID: 19116277; PMCID: PMC2629228.
In vivo protocol:
1. 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. Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent. Proc Natl Acad Sci U S A. 2009 Jan 6;106(1):262-7. doi: 10.1073/pnas.0811325106. Epub 2008 Dec 30. PMID: 19116277; PMCID: PMC2629228.
1: 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. Scaffold-based discovery of indeglitazar, a PPAR
pan-active anti-diabetic agent. Proc Natl Acad Sci U S A. 2009 Jan
6;106(1):262-7. doi: 10.1073/pnas.0811325106. Epub 2008 Dec 30. PubMed PMID:
19116277; PubMed Central PMCID: PMC2629228.
