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AM-5262

Cat. No. M41821
AM-5262 Structure
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Quality Control & Documentation
Biological Activity

AM-5262 is a GPR40 full agonist with an EC50 value of 0.081 μM.

Chemical Information
Molecular Weight 514.63
Formula C33H35FO4
CAS Number 1222088-90-5
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] Louise W Christensen et al. Physiol Rep. Vascular, but not luminal, activation of FFAR1 (GPR40) stimulates GLP-1 secretion from isolated perfused rat small intestine

[2] Maria Hauge et al. Mol Metab. GPR40 (FFAR1) - Combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivo

[3] Yingcai Wang et al. ACS Med Chem Lett. Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles

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