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GCGR antagonist 2
Products Details
Product Description
– 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].
Web ID
– HY-148844
Shipping
– Room temperature
Applications
– Metabolism-sugar/lipid metabolism
Molecular Formula
– C28H26N4O2
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 Number
– 280134-25-0
Molecular Weight
– 450.53
SMILES
– N#CC1=CC(C(N/N=C/C2=CC=CC3=C2C=CN3CC4=C(C)C(C)=CC(C)=C4C)=O)=CC=C1O
Clinical Information
– No Development Reported
Research Area
– Metabolic Disease
Solubility
– 10 mM in DMSO
Target
– GCGR
Pathway
– GPCR/G Protein
Product type
– Reference compound
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