Indeglitazar (Synonyms: PPM 204)

Cat. No.: HY-14817 Purity: 99.11%: FAQs
Data Sheet SDS COA Handling Instructions

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Indeglitazar (PPM 204) is an orally available PPAR pan-agonist for all three PPARα, PPARδ and PPARγ.

For research use only. We do not sell to patients.

Indeglitazar Chemical Structure

CAS No. : 835619-41-5

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10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 370	In-stock	Estimated Time of Arrival: December 31
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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Indeglitazar (PPM 204) is an orally available PPAR pan-agonist for all three PPARα, PPARδ and PPARγ^[1].

IC₅₀ & Target^[1]

PPARα

PPARδ

PPARγ

In Vitro

In an assay of preadipocyte differentiation, measuring in part functional insulin sensitization capability of the cells, Indeglitazar shows an EC₅₀ of 0.32 μM compared with Rosiglitazone, which shows an EC₅₀ of 13 nM, although the maximal response obtained from the 2 compounds is comparable^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

An initial assessment of in vivo activity is carried out using the Zucker rat model of diabetes. The significant lowering of glucose, HbA_1C, triglycerides, and total cholesterol are observed after i.v. treatment with 10 mg/kg Indeglitazar once per day for 3 weeks. Notably, the level of Adiponectin (on day 21) is essentially unchanged in treated vs. untreated animals (4.8 mcg/mL vs. 4.9 mcg/mL), thus the observed reductions in glucose and HbA_1C are achieved in an adiponectin-independent fashion. These differences in the effects of Indeglitazar in vivo may be a consequence of synergy between the 3 PPAR activities or because of the SPPARM profile of the compound, or a combination of these factors. The oral activity of Indeglitazar is assessed in the ob/ob model of diabetes and insulin resistance. Indeglitazar significantly decreases glucose, insulin, triglycerides, and free fatty acid levels^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

389.42

Formula

C₁₉H₁₉NO₆S

CAS No.

835619-41-5

Appearance

Solid

Color

White to gray

SMILES

O=C(O)CCC1=CN(S(=O)(C2=CC=C(OC)C=C2)=O)C3=C1C=C(OC)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (256.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.11%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (255 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Artis DR, et al. 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. [Content Brief]

Kinase Assay ^[1]	The purified PPAR_ LBD protein is diluted to 12 mg/mL and 1mM of Indeglitazar and 2x molar excess of steroid receptor coactivator-1 (SRC-1) peptide are added before crystallization by mixing equal volumes of a protein/compound sample 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 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) before flash-freezing in liquid nitrogen for data collection^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Rats^[1] Indeglitazar is administered once daily i.v. as a solution (10% SolutolHS15,10%ethanol,80%saline) to ZDF/GmiCrl-fa/fa rats. Treatment is initiated at age 7-8 weeks, and blood samples are analyzed before the treatment and 21 days after the treatment. Mice^[1] Ob/ob mouse study. Indeglitazar (10 mg/kg) or Pioglitazone (30 mg/kg) are orally administered to 9-week-old B6.V-Lepob mice for 14 days. Compounds are suspected in 0.5% methylcellulose and 2% Tween 80 before dosing. On the last day, blood is collected for insulin, triglyceride, free fatty acid, and adiponectin measurements. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Artis DR, et al. 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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5679 mL	12.8396 mL	25.6792 mL	64.1980 mL
	5 mM	0.5136 mL	2.5679 mL	5.1358 mL	12.8396 mL
	10 mM	0.2568 mL	1.2840 mL	2.5679 mL	6.4198 mL
	15 mM	0.1712 mL	0.8560 mL	1.7119 mL	4.2799 mL
	20 mM	0.1284 mL	0.6420 mL	1.2840 mL	3.2099 mL
	25 mM	0.1027 mL	0.5136 mL	1.0272 mL	2.5679 mL
	30 mM	0.0856 mL	0.4280 mL	0.8560 mL	2.1399 mL
	40 mM	0.0642 mL	0.3210 mL	0.6420 mL	1.6050 mL
	50 mM	0.0514 mL	0.2568 mL	0.5136 mL	1.2840 mL
	60 mM	0.0428 mL	0.2140 mL	0.4280 mL	1.0700 mL
	80 mM	0.0321 mL	0.1605 mL	0.3210 mL	0.8025 mL
	100 mM	0.0257 mL	0.1284 mL	0.2568 mL	0.6420 mL

Indeglitazar Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Indeglitazar835619-41-5PPM 204PPM204PPM-204PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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Indeglitazar (Synonyms: PPM 204)

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