Glucagon Receptor Antagonist IA potent and selective cell-permeable glucagon receptor antagonist

Glucagon Receptor Antagonist I (CAS 438618-32-7)

Glucagon Receptor Antagonist I | CAS 438618-32-7 is rated 5.0 out of 5 by 1.
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Synonym: N-(3-Cyano-6-(1,1-dimethylpropyl)-4,5,6,7-tetrahydro-1-benzothien-2-yl)-2-ethylbutanamide; hGCGR Antagonist
Application: A potent and selective cell-permeable glucagon receptor antagonist
CAS Number: 438618-32-7
Purity: >95%
Molecular Weight: 346.5
Molecular Formula: C20H30N2OS
* Refer to Certificate of Analysis for lot specific data (including water content).
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Glucagon Receptor Antagonist I is a potent and selective cell-permeable thienyl-amide compound that acts as a competitive antagonist of the glucagon receptor. Exhibits binding to hGCGR with high affinity and prevents its interaction with glucagon (IC50 = 181 nM, KDB = 81 nM, and pA2 = 7.1 in membranes prepared from CHO-hGCGR). Also suppresses glucagon-induced glycogenolysis in human primary hepatocytes and in mice (50 mg/kg, ip).


References

1. Qureshi, S.A., et al. 2004. Diabetes. 53: 3267-3267. PMID: 15561959

Physical State :
Solid
Solubility :
Soluble in DMSO (5 mg/ml), and methanol (5 mg/ml).
Storage :
Store at 4° C
Melting Point :
212.68° C (Predicted)
Boiling Point :
517.78° C at 760 mmHg (Predicted)
Density :
1.08 g/cm3 (Predicted)
Refractive Index :
n20D 1.54 (Predicted)
IC50 :
hGCGR interaction with glucagon: IC50 = 181 nM (membranes prepared from CHO-hGCGR); Glucagon receptor: IC50 = 129 nM (human); human cell lines: IC50 = 129 nM
pK Values :
pKa: 13.46
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
619101
SMILES :
CCC(CC)C(=O)NC1=C(C2=C(S1)CC(CC2)C(C)(C)CC)C#N

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Qureshi Qureshi, SA. et al. (PubMed 15561959) reported that Glucagon Receptor Antagonist I is capable of blocking glucagon-induced glycogenolysis in a dosage-dependent manner. -SCBT Publication Review
Date published: 2015-02-21
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