1. GPCR/G Protein
  2. GPR40

AM-1638 

Cat. No.: HY-13467
Handling Instructions

AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM.

For research use only. We do not sell to patients.

AM-1638 Chemical Structure

AM-1638 Chemical Structure

CAS No. : 1142214-62-7

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM.

IC50 & Target

IC50: 0.16 μM (GPR40/FFA1)[1]

In Vivo

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. Moreover, oral administration of full agonist AM-1638 demonstrates excellent oral bioavailability (mouse, >100%; rat, 72%; and cyno, 71%). AM-1638 exhibits antidiabetic activity in BDF/DIO mice[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9431 mL 9.7157 mL 19.4314 mL
5 mM 0.3886 mL 1.9431 mL 3.8863 mL
10 mM 0.1943 mL 0.9716 mL 1.9431 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]

On the morning of the experiment, Male B6D2F1/J mice are fasted for four hours and body weight and blood glucose levels are measured. Animals are randomized into treatment groups based on these two parameters. Treatments are administered by oral gavage and sixty minutes later, the mice received a 2 g/kg glucose challenge dose by oral gavage (defined as t=0 min). Blood samples are collected at -60, 0, 15, 30, 60, 90 and 120 minutes via tail vein relative to the glucose challenge. Glucose levels are monitored with a glucometer. Plasma insulin is measured using a mouse insulin ELISA[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

514.63

Formula

C₃₃H₃₅FO₄

CAS No.

1142214-62-7

SMILES

FC1=CC=C(OC)C=C1C2=C(C3=CCCC3(C)C)C=C(COC4=CC=CC([[email protected]](C5CC5)CC(O)=O)=C4)C=C2

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
AM-1638
Cat. No.:
HY-13467
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AM-1638

Cat. No.: HY-13467