AMG 837 (calciuM hydrate)
AMG 837 (calciuM hydrate) Basic information
- Product Name:
- AMG 837 (calciuM hydrate)
- Synonyms:
-
- AMG 837 (calciuM hydrate)
- AMG-837 CALCIUM HYDRATE;AMG837 CALCIUM HYDRATE
- AMG-837 calcium salt hydrate
- AMG 837 calcium,FFAR,AMG 837 calcium hydrate,insulin,FFA1,Inhibitor,Free Fatty Acid Receptor,inhibit,glucose,GPR40
- AMG 837 calcium hydrate, 10 mM in DMSO
- Calcium (S)-3-(4-((4'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)methoxy)phenyl)hex-4-ynoate dihydrate
- CAS:
- 1259389-38-2
- MF:
- C26H25CaF3O4
- MW:
- 498.56
- Mol File:
- 1259389-38-2.mol
AMG 837 (calciuM hydrate) Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO: ≥ 42 mg/mL (92.22 mM)
- form
- Solid
- color
- White to off-white
AMG 837 (calciuM hydrate) 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 Cmax 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
AMG 837 (calciuM hydrate)Supplier
- Tel
- 1-631-485-4226; 16314854226
- info@bocsci.com
- Tel
- 0411-62910999 13889544652
- sales@meilune.com
- Tel
- 021-58950125
- info@chemexpress.com
- Tel
- +1 (866) 930-6790
- info@adooq.com
- Tel
- +86 13524779951; 13524779951
- 2075692521@qq.com