280134-25-0
280134-25-0
Chemical Structure
GCGR antagonist 2
- CAS No.: 280134-25-0
- Formula:C28H26N4O2
- Molecular Weight:450.53
IUPAC Name: (E)-3-cyano-4-hydroxy-N'-((1-(2,3,5,6-tetramethylbenzyl)-1H-indol-4-yl)methylene)benzohydrazide
InChIKey: HNTXQDRFWJBZGO-FJEPWZHXSA-N
SMILES: N#CC1=CC(C(N/N=C/C2=CC=CC3=C2C=CN3CC4=C(C)C(C)=CC(C)=C4C)=O)=CC=C1O
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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GCGR antagonist 2 | 98.17% | 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. | ||||||||||||||||||||
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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]
