AS 2034178 |
| Katalog-Nr.GC11467 |
AS 2034178, ein spezifischer und oral aktiver GPR40-Agonist, zeigt eine glukoseabhÄngige InsulinsekretionsverstÄrkung.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1030846-42-4
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 1030846-42-4 | SDF | |
| Chemical Name | 3-(2-fluoro-4-(((1-(2-phenoxyethyl)-1,2,3,4-tetrahydroquinolin-5-yl)methyl)amino)phenyl)propanoic acid | ||
| Canonical SMILES | FC1=C(CCC(O)=O)C=CC(NCC(C=CC=C23)=C2CCCN3CCOC4=CC=CC=C4)=C1 | ||
| Formula | C27H29FN2O3 | M.Wt | 448.53 |
| Löslichkeit | <22.43mg/ml in DMSO; <8.97mg/ml in ethanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2295 mL | 11.1475 mL | 22.2951 mL |
| 5 mM | 0.4459 mL | 2.2295 mL | 4.459 mL |
| 10 mM | 0.223 mL | 1.1148 mL | 2.2295 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
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