GCGR antagonist 2 |
| カタログ番号GC71061 |
GCGR antagonist 2 フラン−2−カルバジドは経口活性グルカゴン受容体拮抗薬である。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 280134-25-0
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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].
GCGR antagonist 2 (0.5 mg/kg for IV, or 2 mg/kg for PO; single dose) shows mean half-lives of 1.11 h and 1.40 h, respectively[1].
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].
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.
[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.
| Cas No. | 280134-25-0 | SDF | |
| Formula | C28H26N4O2 | M.Wt | 450.53 |
| 溶解度 | 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) | Storage | -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 | 2.2196 mL | 11.098 mL | 22.1961 mL |
| 5 mM | 0.4439 mL | 2.2196 mL | 4.4392 mL |
| 10 mM | 0.222 mL | 1.1098 mL | 2.2196 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *