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Insulin efsitora alfa

Cat. No. M24933
Insulin efsitora alfa Structure
Synonym:

LY-3209590

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Biological Activity

Insulin efsitora alfa (LY-3209590) is a selective agonist of insulin receptor (IR). Insulin efsitora alfa is a fusion protein composed of human IR agonists fused with the crystallizable (Fc) domain of human immunoglobulin G2 (IgG2) fragment, with a molecular weight of 64.1 kDa. Insulin efsitora alfa is well tolerated and has potential applications in diabetes.

Chemical Information
CAS Number 2131038-11-2
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] Juliana M Bue-Valleskey, et al. Diabetes Care. Once-Weekly Basal Insulin Fc Demonstrated Similar Glycemic Control to Once-Daily Insulin Degludec in Insulin-Naive Patients With Type 2 Diabetes: A Phase 2 Randomized Control Trial

[2] Christof M Kazda, et al. Diabetes Care. Novel Once-Weekly Basal Insulin Fc Achieved Similar Glycemic Control With a Safety Profile Comparable to Insulin Degludec in Patients With Type 1 Diabetes

[3] Juan Frias, et al. Lancet Diabetes Endocrinol. Safety and efficacy of once-weekly basal insulin Fc in people with type 2 diabetes previously treated with basal insulin: a multicentre, open-label, randomised, phase 2 study

[4] Tim Heise, et al. Diabetes Obes Metab. Pharmacokinetic and pharmacodynamic properties of the novel basal insulin Fc (insulin efsitora alfa), an insulin fusion protein in development for once-weekly dosing for the treatment of patients with diabetes

[5] Julie S Moyers, et al. J Pharmacol Exp Ther. Preclinical Characterization of LY3209590, a Novel Weekly Basal Insulin Fc-Fusion Protein

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