GCGR antagonist 2
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[1][2].
Product Specifications
CAS Number
280134-25-0
UNSPSC
12352005
Target
GCGR
Type
Reference compound
Related Pathways
GPCR/G Protein
Applications
Metabolism-sugar/lipid metabolism
Field of Research
Metabolic Disease
Assay Protocol
https://www.medchemexpress.com/gcgr-antagonist-2.html
Purity
99.76
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
N#CC1=CC(C(N/N=C/C2=CC=CC3=C2C=CN3CC4=C(C)C(C)=CC(C)=C4C)=O)=CC=C1O
Molecular Formula
C28H26N4O2
Molecular Weight
450.53
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
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