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Tesaglitazar

Cat. No. M8514
Tesaglitazar Structure
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Biological Activity

Tesaglitazar is a potent and specific dual PPARα/γ agonist that improves insulin resistance and carbohydrate and lipid metabolism in ob/ob mice and obese Zucker rats.

Chemical Information
Molecular Weight 408.47
Formula C20H24O7S
CAS Number 251565-85-2
Solubility (25°C) DMSO: 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Louis DeRidder, et al. Dendrimer-tesaglitazar conjugate induces a phenotype shift of microglia and enhances β-amyloid phagocytosis

[2] Victoria Osinski, et al. In vivo liposomal delivery of PPARα/γ dual agonist tesaglitazar in a model of obesity enriches macrophage targeting and limits liver and kidney drug effects

[3] Per Lindblom, et al. Tesaglitazar, a dual PPAR-α/γ agonist, hamster carcinogenicity, investigative animal and clinical studies

[4] Sandra L Cox. Tesaglitazar: a promising approach in type 2 diabetes

[5] Niklaus Kamber, et al. Tesaglitazar

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