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Chiglitazar

Cat. No. M30564
Chiglitazar Structure
Synonym:

Carfloglitazar

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Quality Control & Documentation
Biological Activity

Chiglitazar (Carfloglitazar) is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.

Chemical Information
Molecular Weight 572.62
Formula C36H29FN2O4
CAS Number 743438-45-1
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage 4°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Weiping Jia, et al. Sci Bull (Beijing). Chiglitazar monotherapy with sitagliptin as an active comparator in patients with type 2 diabetes: a randomized, double-blind, phase 3 trial (CMAS)

[2] Ralph A DeFronzo. Sci Bull (Beijing). Chiglitazar: a novel pan-PPAR agonist

[3] Yunting Zhou, et al. Front Endocrinol (Lausanne). Comparative Evaluation of Chiglitazar and Sitagliptin on the Levels of Retinol-Binding Protein 4 and Its Correlation With Insulin Resistance in Patients With Type 2 Diabetes

[4] Yuming Wang, et al. Diabetes Res Clin Pract. Effect of chiglitazar and sitagliptin on glucose variations, insulin resistance and inflammatory-related biomarkers in untreated patients with type 2 diabetes

[5] Emma D Deeks. Drugs. Chiglitazar: First Approval

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