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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
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 438.44
Formula C26H21F3O3
CAS Number 865231-46-5
Purity >98%
Solubility DMSO
Storage at -20°C
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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