AMG 837 (calciuM hydrate)

Product NameAMG 837 (calciuM hydrate)
CAS1259389-38-2
MFC26H25CaF3O4
MW498.56
EINECS
MOL File1259389-38-2.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	DMSO: ≥ 42 mg/mL (92.22 mM)
form	Solid
color	White to off-white

Usage And Synthesis

Uses

AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 calcium hydrate inhibits specific [3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 calcium hydrate could enhance insulin secretion and lower glucose levels in rodents[1][2][3]. AMG 837 (calcium hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

in vivo

AMG 837 (0.03-0.3 mg/kg; p.o. once daily for 21 days) reduces glucose levels and increases insulin levels following glucose challenge in vivo^[1].
AMG 837 (0.03-0.3 mg/kg; a single p.o.) improves glucose tolerance and enhances insulin secretion in Sprague-Dawley rats^[1].
AMG 837 (0.5 mg/kg; p.o.) displays excellent oral bioavailability (F=84%) and a total plasma C_max of 1.4 μM^[1].

Animal Model:	8-week old Zucker Fatty Rats^[1]
Dosage:	0.03, 0.1, 0.3 mg/kg
Administration:	Oral gavage once daily for 21 days
Result:	Decreased glucose AUC values during the glucose tolerance test (GTT) to 7%, 15%, and 25% at 0.03, 0.1 and 0.3 mg/kg, respectively. Increased insulin levels in the mid- and high-dose groups. Not affected body weights during the 21-day treatment.

Animal Model:	8-week old Sprague-Dawley rats^[1]
Dosage:	0.03, 0.1, 0.3 mg/kg
Administration:	A single p.o. administration
Result:	Reduced the post-prandial glucose with the half-maximal dose of 0.05 mg/kg.

References

[1] Daniel CHL, et, al. AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents. PLoS One. 2011; 6(11): e27270. DOI:10.1371/journal.pone.0027270
[2] Houze JB, et, al. AMG 837: a potent, orally bioavailable GPR40 agonist. Bioorg Med Chem Lett. 2012 Jan 15; 22(2): 1267-70. DOI:10.1016/j.bmcl.2011.10.118
[3] Daniel CHL, et, al. Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptor. Mol Pharmacol. 2012 Nov;82(5):843-59. DOI:10.1124/mol.112.079640

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