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GLP-1 receptor agonist 13

Cat. No. M41835
GLP-1 receptor agonist 13 Structure
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Biological Activity

GLP-1 receptor agonist 13 is a glucagon GLP-1 receptor agonist with EC50 of 76 nM.

Chemical Information
Molecular Weight 496.94
Formula C25H23ClF2N6O
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] Julien Bezin et al. Diabetes Care. GLP-1 Receptor Agonists and the Risk of Thyroid Cancer

[2] Daniel Weghuber et al. N Engl J Med. Once-Weekly Semaglutide in Adolescents with Obesity

[3] Michael A Nauck et al. Cardiovasc Diabetol. Tirzepatide, a dual GIP/GLP-1 receptor co-agonist for the treatment of type 2 diabetes with unmatched effectiveness regrading glycaemic control and body weight reduction

[4] Melissa K Thomas et al. J Clin Endocrinol Metab. Dual GIP and GLP-1 Receptor Agonist Tirzepatide Improves Beta-cell Function and Insulin Sensitivity in Type 2 Diabetes

[5] Tamer Coskun et al. Mol Metab. LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept

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