1. Cell Cycle/DNA Damage
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  3. Indeglitazar

Indeglitazar (Synonyms: PPM 204)

Cat. No.: HY-14817 Purity: 99.42%
Handling Instructions

Indeglitazar is an orally available peroxisome proliferator-activated receptor (PPAR) pan-agonist for all three PPAR subtypes alpha (α), delta (δ) and gamma (γ).

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

Indeglitazar Chemical Structure

Indeglitazar Chemical Structure

CAS No. : 835619-41-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 69 In-stock
Estimated Time of Arrival: December 31
1 mg USD 50 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 100 In-stock
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25 mg USD 200 In-stock
Estimated Time of Arrival: December 31
50 mg USD 300 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
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Description

Indeglitazar is an orally available peroxisome proliferator-activated receptor (PPAR) pan-agonist for all three PPAR subtypes alpha (α), delta (δ) and gamma (γ).

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].

In Vivo

An initial assessment of in vivo activity is carried out using the Zucker rat model of diabetes. The significant lowering of glucose, HbA1C, 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 HbA1C 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].

Clinical Trial
Molecular Weight

389.42

Formula

C₁₉H₁₉NO₆S

CAS No.

835619-41-5

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33 mg/mL (84.74 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
References
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

Purity: 99.42%

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KeyWords:

Indeglitazar | PPM 204 | PPM204 | PPM-204 | PPAR | Peroxisome proliferator-activated receptors | Inhibitor | inhibitor | inhibit

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