GLP-1R agonist 2
Based on 1 Customer Validation
GLP-1R agonist 2 (compound 2) is an effective GLP-1R agonist that exerts its activating effect by forming hydrogen bonds with the Tyr42, Cys71, and Ser84 residues of GLP-1R. GLP-1R agonist 2 has the potential for research in metabolic diseases such as type 2 diabetes and obesity.
For research use only. We do not sell to patients.
- Purity: 99.57%
- CAS No.: 281209-71-0
- Formula: C13H15Cl2N3O2S
- Molecular Weight:348.25
-
Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Biological Activity
GLP-1R agonist 2 (100 nM, 1,000 nM) activates GLP-1 receptor-mediated cAMP production, with an EC50 of 101 nM, but exhibits a self-limiting effect at high concentrations[2]. GLP-1R agonist 2 (100 nM) enhances GLP-1 binding to the GLP-1 receptor, reducing the Kd value from 0.51 nM to 0.19 nM[2]. GLP-1R agonist 2 (100 nM, 1,000 nM) promotes glucose-dependent insulin secretion in CD1 mouse islets, and this effect is dependent on the GLP-1 receptor. Specifically, at concentrations of 100 nM and 1,000 nM, GLP-1R agonist 2 significantly enhances 10 mM glucose-induced insulin secretion, similar to GLP-1, and this effect is abolished in islets from GLP-1 receptor knockout mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 281209-71-0
-
Appearance Solid
-
Molecular Weight 348.25
-
Formula C13H15Cl2N3O2S
-
Color Light yellow to yellow
-
SMILES
O=S(C1=NC2=CC(Cl)=C(Cl)C=C2N=C1NC(C)(C)C)(C)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 25 mg/mL (71.79 mM; ultrasonic and warming and heat to 60°C; 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)
Purity & Documentation
-
Data Sheet (277 KB)
-
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
-
Handling Instructions (2659 KB)
References
[1]. Girdhar K, et al. Novel insights into the dynamics behavior of glucagon-like peptide-1 receptor with its small molecule agonists. J Biomol Struct Dyn. 2019 Sep;37(15):3976-3986. [Content Brief]
[2]. Knudsen LB, et al. Small-molecule agonists for the glucagon-like peptide 1 receptor. Proc Natl Acad Sci U S A. 2007 Jan 16;104(3):937-42. [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 | 2.8715 mL | 14.3575 mL | 28.7150 mL | 71.7875 mL |
| 5 mM | 0.5743 mL | 2.8715 mL | 5.7430 mL | 14.3575 mL | |
| 10 mM | 0.2872 mL | 1.4358 mL | 2.8715 mL | 7.1788 mL | |
| 15 mM | 0.1914 mL | 0.9572 mL | 1.9143 mL | 4.7858 mL | |
| 20 mM | 0.1436 mL | 0.7179 mL | 1.4358 mL | 3.5894 mL | |
| 25 mM | 0.1149 mL | 0.5743 mL | 1.1486 mL | 2.8715 mL | |
| 30 mM | 0.0957 mL | 0.4786 mL | 0.9572 mL | 2.3929 mL | |
| 40 mM | 0.0718 mL | 0.3589 mL | 0.7179 mL | 1.7947 mL | |
| 50 mM | 0.0574 mL | 0.2872 mL | 0.5743 mL | 1.4358 mL | |
| 60 mM | 0.0479 mL | 0.2393 mL | 0.4786 mL | 1.1965 mL |