GCGR antagonist 2
Based on 1 Customer Validation
GCGR antagonist 2, a Furan-2-carbohydrazide, is an orally active glucagon receptor antagonist. GCGR antagonist 2 binds to hGluR with an Kd value of 2.3 nM, and inhibits rat receptor with an IC50 value of 0.43 nM. GCGR antagonist 2 inhibits glucagon-stimulated glycogenolysis.
For research use only. We do not sell to patients.
- Purity: 98.17%
- CAS No.: 280134-25-0
- Formula: C28H26N4O2
- Molecular Weight:450.53
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
GCGR antagonist 2 (compound 74) (25 nM, 250 nM, and 2500 nM; 70 min) inhibits 5 nM glucagon-induced glycogenolysis in primary rat hepatocytes, with an IC50 value of 160 nM[1].
GCGR antagonist 2 (25 nM, 250 nM, and 2500 nM; 60 min) inhibits glucagon-stimulated cAMP level with the recombinant human glucagon receptor in BHK cells[1].
GCGR antagonist 2 (1 nM, 10 nM, and 100 nM; 60 min) inhibits glucagon-stimulated cAMP level with isolated rat liver glucagon receptor in BHK cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GCGR antagonist 2 (0 mg/kg, 3 mg/kg, and 10 mg/kg; p.o.) at least partly, inhibits the action of the endogenous glucagon responsible for maintenance of euglycemia in glucagon-challenged Sprague-Dawley rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 280134-25-0
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Appearance Solid
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Molecular Weight 450.53
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Formula C28H26N4O2
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Color White to off-white
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SMILES
N#CC1=CC(C(N/N=C/C2=CC=CC3=C2C=CN3CC4=C(C)C(C)=CC(C)=C4C)=O)=CC=C1O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (221.96 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. 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. 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: 2.5 mg/mL (5.55 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
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.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Madsen P, et al. Optimization of alkylidene hydrazide based human glucagon receptor antagonists. Discovery of the highly potent and orally available 3-cyano-4-hydroxybenzoic acid [1-(2,3,5,6-tetramethylbenzyl)-1H-indol-4-ylmethylene]hydrazide. J Med Chem. 2002 Dec 19;45(26):5755-75. [Content Brief]
[2]. Hasegawa F, et al. Discovery of furan-2-carbohydrazides as orally active glucagon receptor antagonists. Bioorg Med Chem Lett. 2014 Sep 1;24(17):4266-70. [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. 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 | 2.2196 mL | 11.0980 mL | 22.1961 mL | 55.4902 mL |
| 5 mM | 0.4439 mL | 2.2196 mL | 4.4392 mL | 11.0980 mL | |
| 10 mM | 0.2220 mL | 1.1098 mL | 2.2196 mL | 5.5490 mL | |
| 15 mM | 0.1480 mL | 0.7399 mL | 1.4797 mL | 3.6993 mL | |
| 20 mM | 0.1110 mL | 0.5549 mL | 1.1098 mL | 2.7745 mL | |
| 25 mM | 0.0888 mL | 0.4439 mL | 0.8878 mL | 2.2196 mL | |
| 30 mM | 0.0740 mL | 0.3699 mL | 0.7399 mL | 1.8497 mL | |
| 40 mM | 0.0555 mL | 0.2775 mL | 0.5549 mL | 1.3873 mL | |
| 50 mM | 0.0444 mL | 0.2220 mL | 0.4439 mL | 1.1098 mL | |
| 60 mM | 0.0370 mL | 0.1850 mL | 0.3699 mL | 0.9248 mL | |
| 80 mM | 0.0277 mL | 0.1387 mL | 0.2775 mL | 0.6936 mL | |
| 100 mM | 0.0222 mL | 0.1110 mL | 0.2220 mL | 0.5549 mL |
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