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AMG-837

Cat. No. M2384
AMG-837 Structure
Size Price Availability Quantity
5mg USD 140  USD140 In stock
10mg USD 220  USD220 In stock
25mg USD 450  USD450 In stock
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Quality Control & Documentation
Biological Activity

AMG 837 is a potent, orally bioavailable GPR40 agonist with EC50 of 14 nM.

Customer Product Validations & Biological Datas
Source Physiol Rep (2015). Figure 3. AMG-837
Method Hormone measurement
Cell Lines rat small intestine
Concentrations 10 μmol/L
Incubation Time -
Results Intergroup comparisons between LA, TAK-875, AMG 837, and DMSO stimulations showed that only the GLP-1 response induced by vascular AMG 837 was significantly different from the vehicle control
Chemical Information
Molecular Weight 438.44
Formula C26H21F3O3
CAS Number 865231-46-5
Solubility (25°C) DMSO
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] Xihao Chang, et al. Collective synthesis of acetylenic pharmaceuticals via enantioselective Nickel/Lewis acid-catalyzed propargylic alkylation

[2] Sameer Mohammad. GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus: Benefits and Challenges

[3] Jonathan B Houze, et al. AMG 837: a potent, orally bioavailable GPR40 agonist

[4] Daniel C-H Lin, et al. AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents

[5] Ryo Yazaki, et al. Enantioselective synthesis of a GPR40 agonist AMG 837 via catalytic asymmetric conjugate addition of terminal alkyne to α,β-unsaturated thioamide

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