Indeglitazar

Research use only, not for human use.

Indeglitazar is orally available pan-agonist of PPAR (PPAR subtypes alpha (α), delta (δ), and gamma (γ)).

Indeglitazar is orally available pan-agonist of PPAR (PPAR subtypes alpha (α), delta (δ), and gamma (γ)).(In Vitro):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, in an assay of preadipocyte differentiation.(In Vivo):In Zucker rat model of diabetes, Indeglitazar (10 mg/kg; i.v.) significantly lowers the levels of glucose, HbA1C, triglycerides. In the ob/ob model of diabetes and insulin resistance, Indeglitazar significantly decreases glucose, insulin, triglycerides, and free fatty acid levels. The level of Adiponectin (day 21) is essentially unchanged, thus the observed reductions in glucose and HbA1C are achieved in an adiponectin-independent fashion.

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.

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.

PPM 204

Metabolic Enzyme/Protease

PPAR

ABCG2| Antibacterial| Antibiotic| BCRP

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835619-41-5

389.42

C19H19NO6S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (256.79 mM)

O=C(O)CCC1=CN(C=2C=CC(OC)=CC21)S(=O)(=O)C3=CC=C(OC)C=C3

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(-20℃)

With Ice Pack

≥ 2 years