| Identification | Back Directory | [Name]
AS2034178 | [CAS]
1030846-42-4 | [Synonyms]
AS2034178
2-Fluoro-4-[[[1,2,3,4-Tetrahydro-1-(2-phenoxyethyl)-5-quinolinyl]methyl]amino]benzenepropanoic acid
Benzenepropanoic acid, 2-fluoro-4-[[[1,2,3,4-tetrahydro-1-(2-phenoxyethyl)-5-quinolinyl]methyl]amino]- | [Molecular Formula]
C27H29FN2O3 | [MDL Number]
MFCD28133388 | [MOL File]
1030846-42-4.mol | [Molecular Weight]
448.53 |
| Chemical Properties | Back Directory | [Boiling point ]
657.9±55.0 °C(Predicted) | [density ]
1.240±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
<22.43mg/ml in DMSO; <8.97mg/ml in ethanol | [form ]
solid | [pka]
4.76±0.10(Predicted) | [color ]
White |
| Hazard Information | Back Directory | [Uses]
AS 2034178 is used in the synthetic preparation of quinolines and related compounds as GPR40 agonists, some of which are potentially useful in the treatment of diabetes. | [Biological Activity]
as2034178 is a gpr40 agonist [1] with an hec50 value of 380 nm [2].gpr40 is a receptor of free fatty acid. it regulates glucose-dependent insulin secretion [1].as2034178 can improve glucose homeostasis and maintain or enhance islet beta cell functions [3]. as2034178 demonstrated highly and dose-dependently increase in intracellular ca2+ levels [1]. the maximum efficacy of the increase in ca2+ was nearly equal to that of an endogenous ligand of gpr40, namely linolenic acid. but the potency of as2034178 was much higher than that of linolenic acid. human gpr41-, gpr43-, gpr119-, and gpr120-overexpressing cho cells were developed to evaluate the increase of intracellular ca2+ concentration caused by as2034178. only gpr40-expressing cells showed increased intracellular ca2+. in pancreas b-cell–derived min6 cells, as2034178 dose-dependently and significantly induced insulin secretion only under high-glucose conditions (22.4 mm) [1].in ob/ob mice, chronic treatment with as2034178 significantly improved whole-body glucose metabolism, insulin, hba1c, and pancreatic insulin levels [2]. in normal mice, as2034178 at 0.3 to 10 mg/kg dose-dependently induced the suppression of plasma-glucose increases after oral administration with glucose, and the area decrease under the plasma glucose concentration-time curve was significant at doses over 1 mg/kg. after oral glucose administration, plasma insulin levels increased and at 5 minutes after glucose administration were dose-dependently and significantly increased at as2034178 dosages over 3 mg/kg [1]. | [References]
[1]. tanaka h, yoshida s, oshima h, et al. chronic treatment with novel gpr40 agonists improve whole-body glucose metabolism based on the glucose-dependent insulin secretion[j]. journal of pharmacology and experimental therapeutics, 2013, 346(3): 443-452.
[2]. defossa e, wagner m. recent developments in the discovery of ffa1 receptor agonists as novel oral treatment for type 2 diabetes mellitus[j]. bioorganic & medicinal chemistry letters, 2014, 24(14): 2991-3000.
[3]. milligan g, alvarez-curto e, watterson kr, et al. characterizing pharmacological ligands to study the long-chain fatty acid receptors gpr40/ffa1 and gpr120/ffa4[j]. british journal of pharmacology, 2015, 172(13): 3254-3265. |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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