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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

Frequently Asked Questions

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