Indeglitazar
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MedKoo CAT#: 319853

CAS#: 835619-41-5

Description: Indeglitazar, also known as PPM-204 and PLX-204, is an orally available peroxisome proliferator-activated receptor (PPAR) pan-agonist for all three PPAR subtypes alpha (α), delta (δ) and gamma under development for for Type 2 diabetes mellitus (T2DM).


Chemical Structure

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Indeglitazar
CAS# 835619-41-5

Theoretical Analysis

MedKoo Cat#: 319853
Name: Indeglitazar
CAS#: 835619-41-5
Chemical Formula: C19H19NO6S
Exact Mass: 389.09
Molecular Weight: 389.422
Elemental Analysis: C, 58.60; H, 4.92; N, 3.60; O, 24.65; S, 8.23

Price and Availability

Size Price Availability Quantity
100mg USD 450
200mg USD 750
500mg USD 1250
1g USD 2150
2g USD 3650
Bulk inquiry

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

Appearance: Solid powder

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

More Info:

Product Data:
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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 100.0 256.79

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.

Recalculate based on batch purity %
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.

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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.