AS 2034178GPR40 agonist CAS# 1030846-42-4 |
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Quality Control & MSDS
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Chemical structure
3D structure
| Cas No. | 1030846-42-4 | SDF | Download SDF |
| PubChem ID | 24808572 | Appearance | Powder |
| Formula | C27H29FN2O3 | M.Wt | 448.53 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 50 mM in DMSO and to 20 mM in ethanol | ||
| Chemical Name | 3-[2-fluoro-4-[[1-(2-phenoxyethyl)-3,4-dihydro-2H-quinolin-5-yl]methylamino]phenyl]propanoic acid | ||
| SMILES | C1CC2=C(C=CC=C2N(C1)CCOC3=CC=CC=C3)CNC4=CC(=C(C=C4)CCC(=O)O)F | ||
| Standard InChIKey | VENOXIKBBUVHRY-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C27H29FN2O3/c28-25-18-22(13-11-20(25)12-14-27(31)32)29-19-21-6-4-10-26-24(21)9-5-15-30(26)16-17-33-23-7-2-1-3-8-23/h1-4,6-8,10-11,13,18,29H,5,9,12,14-17,19H2,(H,31,32) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Selective free fatty acid receptor 1 (FFA1/GPR40) agonist. Exhibits selectivity for GPR40 over GPR41, GPR43, GPR119, GPR120 and PPARγ. Induces glucose-dependent insulin secretion in pancreatic MIN6 cells and in vivo. Enhances insulin sensitivity in a type 2 diabetes model in vivo. Orally available. |
AS 2034178 Dilution Calculator
AS 2034178 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2295 mL | 11.1475 mL | 22.2951 mL | 44.5901 mL | 55.7376 mL |
| 5 mM | 0.4459 mL | 2.2295 mL | 4.459 mL | 8.918 mL | 11.1475 mL |
| 10 mM | 0.223 mL | 1.1148 mL | 2.2295 mL | 4.459 mL | 5.5738 mL |
| 50 mM | 0.0446 mL | 0.223 mL | 0.4459 mL | 0.8918 mL | 1.1148 mL |
| 100 mM | 0.0223 mL | 0.1115 mL | 0.223 mL | 0.4459 mL | 0.5574 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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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Chronic treatment with novel GPR40 agonists improve whole-body glucose metabolism based on the glucose-dependent insulin secretion.[Pubmed:23853170]
J Pharmacol Exp Ther. 2013 Sep;346(3):443-52.
GPR40 is a free fatty acid receptor that has been shown to regulate glucose-dependent insulin secretion. This study aimed to discover novel GPR40 agonists and investigate the whole-body effect on glucose metabolism of GPR40 activation using these novel GPR40 agonists. To identify novel GPR40-specific agonists, we conducted high-throughput chemical compound screening and evaluated glucose-dependent insulin secretion. To investigate the whole-body effect on glucose metabolism of GPR40 activation, we conducted repeat administration of the novel GPR40 agonists to diabetic model ob/ob mice and evaluated metabolic parameters. To characterize the effect of the novel GPR40 agonists more deeply, we conducted an insulin tolerance test and a euglycemic-hyperinsulinemic clamp test. As a result, we discovered the novel GPR40-specific agonists, including AS2034178 [bis{2-[(4-{[4'-(2-hydroxyethoxy)-2'-methyl[1,1'-biphenyl]-3-yl]methoxy}phenyl)me thyl]-3,5-dioxo-1,2,4-oxadiazolidin-4-ide} tetrahydrate], and found that its exhibited glucose-dependent insulin secretion enhancement both in vitro and in vivo. In addition, the compounds also decreased plasma glucose and HbA1c levels after repeat administration to ob/ob mice, with favorable oral absorption and pharmacokinetics. Repeat administration of AS2034178 enhanced insulin sensitivity in an insulin tolerance test and a euglycemic-hyperinsulinemic clamp test. These results indicate that improvement of glucose-dependent insulin secretion leads the improvement of whole-body glucose metabolism chronically. In conclusion, AS2034178 and other GPR40 agonists may become useful therapeutics in the treatment of type 2 diabetes mellitus.
