AS1269574
Based on 1 publication(s) in Google Scholar
AS1269574 is a potent, orally available GPR119 agonist, with an EC50 of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates TRPA1 cation channels to stimulate glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induces glucose-dependent insulin secretion from pancreatic β-cells only under high-glucose conditions. AS1269574 has the potential for the research of type 2 diabetes.
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- Purity: 99.84%
- CAS No.: 330981-72-1
- 화학식: C13H14BrN3O
- 분자량:308.17
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) AS1269574
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Biological Activity
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GPR119 |
TRPA1 |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
2.5 μM
Compound: 9a
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Agonist activity at human GPR119 expressed in HEK293 cells co-transfected with pCRE-Luc assessed as induction in cAMP level after 6 hrs by luciferase reporter gene assay
Agonist activity at human GPR119 expressed in HEK293 cells co-transfected with pCRE-Luc assessed as induction in cAMP level after 6 hrs by luciferase reporter gene assay
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[PMID: 22365911] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Eight-week-old ICR mice[1]
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Dosage:100 mg/kg
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Administration:P.o.
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Result:Sgnificantly reduced the blood glucose AUC after 2 h (AUC0-2h) of administration. Similarly, plasma insulin AUC0-2h was significantly higher in the mice.
Chemical Information
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CAS No. 330981-72-1
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Appearance Solid
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분자량 308.17
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화학식 C13H14BrN3O
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Color Light yellow to yellow
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SMILES
OCCNC1=NC(C2=CC=C(Br)C=C2)=NC(C)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Structure
2026 Jun 10:S0969-2126(26)00153-X. PMID: 42269610
용액&용해도
DMSO : 250 mg/mL (811.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.75 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.75 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (271 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Yoshida S, et al. Identification of a novel GPR119 agonist, AS1269574, with in vitro and in vivo glucose-stimulated insulin secretion. Biochem Biophys Res Commun. 2010;400(3):437-441. [Content Brief]
[2]. Chepurny OG, et al. GPR119 Agonist AS1269574 Activates TRPA1 Cation Channels to Stimulate GLP-1 Secretion. Mol Endocrinol. 2016;30(6):614-629. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2450 mL | 16.2248 mL | 32.4496 mL | 81.1241 mL |
| 5 mM | 0.6490 mL | 3.2450 mL | 6.4899 mL | 16.2248 mL | |
| 10 mM | 0.3245 mL | 1.6225 mL | 3.2450 mL | 8.1124 mL | |
| 15 mM | 0.2163 mL | 1.0817 mL | 2.1633 mL | 5.4083 mL | |
| 20 mM | 0.1622 mL | 0.8112 mL | 1.6225 mL | 4.0562 mL | |
| 25 mM | 0.1298 mL | 0.6490 mL | 1.2980 mL | 3.2450 mL | |
| 30 mM | 0.1082 mL | 0.5408 mL | 1.0817 mL | 2.7041 mL | |
| 40 mM | 0.0811 mL | 0.4056 mL | 0.8112 mL | 2.0281 mL | |
| 50 mM | 0.0649 mL | 0.3245 mL | 0.6490 mL | 1.6225 mL | |
| 60 mM | 0.0541 mL | 0.2704 mL | 0.5408 mL | 1.3521 mL | |
| 80 mM | 0.0406 mL | 0.2028 mL | 0.4056 mL | 1.0141 mL | |
| 100 mM | 0.0324 mL | 0.1622 mL | 0.3245 mL | 0.8112 mL |
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