Indeglitazar (PPM 204 and PLX 204)

Alias: PLX-204; PLX204; PLX 204; PPM-204; PPM204; PPM 204

Cat No.:V5144 Purity: ≥98%

COA Product Data Instructions for use SDS

Indeglitazar (formerly PPM-204 and PLX-204) is a novel, potent and orally bioavailable peroxisome proliferator-activated receptor (PPAR) pan-agonist for all three PPAR subtypes alpha (α), delta (δ) and gamma (γ).

Indeglitazar (PPM 204 and PLX 204) Chemical Structure CAS No.: 835619-41-5
Product category: PPAR

This product is for research use only, not for human use. We do not sell to patients.

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

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Science Trans Med 2023, 15: eadd7872.

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Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Indeglitazar (formerly PPM-204 and PLX-204) is a novel, potent and orally bioavailable pan-agonist for the three PPAR subtypes, alpha (α), delta (δ), and gamma (γ), of the peroxisome proliferator-activated receptor (PPAR). Indeglitazar is a medication being developed to treat Type 2 diabetes (T2DM).

Biological Activity I Assay Protocols (From Reference)

Targets	PPARα; PPARδ; PPARγ
ln Vitro	In a preadipocyte differentiation assay, which evaluates the cells' functional insulin sensitization ability, Indeglitazar exhibits an EC50 of 0.32 μM while Rosiglitazone displays an EC50 of 13 nM. Despite this, the two compounds yield comparable maximal responses[1].
ln Vivo	The Zucker rat model of diabetes is used to perform a preliminary evaluation of in vivo activity. Following intravenous treatment with 10 mg/kg Indeglitazar once daily for three weeks, there is a significant reduction in glucose, HbA_1C, triglycerides, and total cholesterol. The observed decreases in glucose and HbA_1C are accomplished in an adiponectin-independent manner because, remarkably, the level of Adiponectin (on day 21) is essentially unchanged in treated vs. untreated animals (4.8 mcg/mL vs. 4.9 mcg/mL). These variations in Indeglitazar's in vivo effects could be the result of interactions between the compound's three PPAR activities, its SPPARM profile, or a combination of these factors. Using the ob/ob model of diabetes and insulin resistance, the oral activity of Indeglitazar is evaluated. Triglycerides, free fatty acid, insulin, and glucose are all markedly reduced by indglitazar[1].
Enzyme Assay	Before crystallization, equal volumes of a protein or compound sample are mixed with reservoir solution containing 27% polyethylene glycol (PEG) 4000, 0.1 M 2-(bis-(2-hydroxy-ethyl)-amino)-2-hydroxymethyl-propane-1,3-diol (BisTris) buffer at pH 6.5, 0.2 M ammonium acetate, and 5% glycerol. The purified PPAR_ LBD protein is diluted to 12 mg/mL, and 1 mM of Indeglitazar and a 2x molar excess of steroid receptor coactivator-1 (SRC-1) peptide are added prior to crystallization. Before being flash-frozen in liquid nitrogen for data collection, the crystals are soaked in cryo-protective buffer (30% PEG 4000, 0.1 M BisTris buffer at pH 6.5, 0.2 M ammonium acetate, and 5% glycerol)[1].
Animal Protocol	Rats: To ZDF/GmiCrl-fa/fa rats, indentistazar is given intravenously (10% SolutolHS15, 10% ethanol, 80% saline) once a day. Blood samples are examined 21 days before and after the treatment, which is started at 7-8 weeks of age. Mice: Ob/ob mouse experiment. Nine-week-old B6.V-Lepob mice are given either indagoglitazar (10 mg/kg) or pioglitazone (30 mg/kg) orally for a period of 14 days. Prior to dosing, compounds are suspected in 0.5% methylcellulose and 2% Tween 80. Blood is drawn on the final day to measure adiponectin, insulin, triglycerides, and free fatty acids.
References	[1]. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C19H19NO6S
Molecular Weight	389.42226
Exact Mass	389.09
Elemental Analysis	C, 58.60; H, 4.92; N, 3.60; O, 24.65; S, 8.23
CAS #	835619-41-5
Related CAS #	835619-41-5
Appearance	Solid powder
SMILES	COC1=CC=C(C=C1)S(=O)(=O)N2C=C(C3=C2C=CC(=C3)OC)CCC(=O)O
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)
Chemical Name	3-[5-methoxy-1-(4-methoxyphenyl)sulfonylindol-3-yl]propanoic acid
Synonyms	PLX-204; PLX204; PLX 204; PPM-204; PPM204; PPM 204
HS Tariff Code	2934.99.9001
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)	DMSO: ~100 mg/mL (~256.8 mM)
Solubility (In Vivo)	Solubility in Formulation 1: ≥ 2.5 mg/mL (6.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.42 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More Solubility in Formulation 3: ≥ 2.5 mg/mL (6.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.)

Solubility (In Vitro)

DMSO: ~100 mg/mL (~256.8 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.42 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

View More

Solubility in Formulation 3: ≥ 2.5 mg/mL (6.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.5679 mL	12.8396 mL	25.6792 mL
	5 mM	0.5136 mL	2.5679 mL	5.1358 mL
	10 mM	0.2568 mL	1.2840 mL	2.5679 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

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Concentration (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00447629	Completed	Drug: PPM-204	Diabetes Mellitus	Wyeth is now a wholly owned subsidiary of Pfizer	January 2007	Phase 1
NCT00448032	Completed	Drug: PPM-204	Diabetes Mellitus	Wyeth is now a wholly owned subsidiary of Pfizer	November 2006	Phase 1
NCT00425919	Terminated	Drug: PPM-204	Diabetes Mellitus	Wyeth is now a wholly owned subsidiary of Pfizer	January 2007	Phase 2

Biological Data

Discovery and structural characterization of indeglitazar.Proc Natl Acad Sci U S A. 2009 Jan 6;106(1):262-7.
Cellular activity of indeglitazar and its effect on the expression of adiponectin and in vivo adiponectin response.Proc Natl Acad Sci U S A. 2009 Jan 6;106(1):262-7.

In vivo effect on body weight. (AandB) Effects of indeglitazar and fenofibrate on body weight and triglyceride levels in a hamster DIO model after 14 days of oral dosing.Proc Natl Acad Sci U S A. 2009 Jan 6;106(1):262-7.