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Cat. No. M21826
AM-1638 Structure


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Biological Activity

AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM. AM-1638 exhibits moderate cross-species plasma clearance and volume of distribution, resulting in plasma half-lives suitable for evaluation of its antidiabetic properties in mouse, rat, and cynomologus monkey. AM-1638 exhibits antidiabetic activity in BDF/DIO mice. Moreover, oral administration of full agonist AM-1638 demonstrates excellent oral bioavailability (mouse, >100%; rat, 72%; and cyno, 71%).

Chemical Information
Molecular Weight 514.63
Formula C33H35FO4
CAS Number 1142214-62-7
Solubility (25°C) DMSO 90 mg/mL
Storage 4°C, protect from light
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.


[1] Sean P Brown, et al. ACS Med Chem Lett. Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates

[2] Sanath K Meegalla, et al. Bioorg Med Chem Lett. Discovery of a novel potent GPR40 full agonist

[3] Xiaohui Du, et al. ACS Med Chem Lett. Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists

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

[5] Sean P Brown, et al. ACS Med Chem Lett. Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist

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Keywords: AM-1638, AM1638 supplier, GPR, inhibitors, activators

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