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Sergliflozin etabonate

Cat. No. M30056
Sergliflozin etabonate Structure
Synonym:

GW-869682X

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Biological Activity

Sergliflozin etabonate (GW-869682X) is a potent and orally active sodium glucose cotransporter (SGLT2) inhibitor. Sergliflozin etabonate shows antidiabetic and antihyperglycemic effects. Sergliflozin etabonate significantly reduces non-fasting blood glucose levels in diabetic mice. Sergliflozin etabonate has the potential for the research of diabetes.

Chemical Information
Molecular Weight 448.46
Formula C23H28O9
CAS Number 408504-26-7
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Antonella Napolitano, et al. J Clin Transl Endocrinol. Exploring glycosuria as a mechanism for weight and fat mass reduction. A pilot study with remogliflozin etabonate and sergliflozin etabonate in healthy obese subjects

[2] Elizabeth K Hussey, et al. J Clin Pharmacol. Multiple-dose pharmacokinetics and pharmacodynamics of sergliflozin etabonate, a novel inhibitor of glucose reabsorption, in healthy overweight and obese subjects: a randomized double-blind study

[3] Elizabeth K Hussey, et al. J Clin Pharmacol. Single-dose pharmacokinetics and pharmacodynamics of sergliflozin etabonate, a novel inhibitor of glucose reabsorption, in healthy volunteers and patients with type 2 diabetes mellitus

[4] Kenji Katsuno, et al. Eur J Pharmacol. Long-term treatment with sergliflozin etabonate improves disturbed glucose metabolism in KK-A(y) mice

[5] Yoshikazu Fujimori, et al. Eur J Pharmacol. Sergliflozin etabonate, a selective SGLT2 inhibitor, improves glycemic control in streptozotocin-induced diabetic rats and Zucker fatty rats

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Keywords: Sergliflozin etabonate, GW-869682X supplier, SGLT, inhibitors, activators

 
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