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Cat.No. 2311 - L-168,049 | C24H20BrClN2O | CAS No. 191034-25-0
Description: Potent, orally active human glucagon receptor antagonist
Chemical Name: 4-[3-(5-Bromo-2-propoxyphenyl)-5-(4-chlorophenyl)-1H-pyrrol-2-yl]pyridine
Purity: ≥99% (HPLC)

Biological Activity

Very potent and selective, non-competitive antagonist of the human glucagon receptor (hGR). Binds with high affinity to human GR (IC50 = 3.7 nM), and moderate affinity to murine and canine GRs (IC50 values are 63 and 60 nM respectively). In contrast, displays poor affinity for rat, guinea pig, and rabbit glucagon receptors (IC50 > 1 μM). In functional studies, inhibits glucagon-stimulated cAMP synthesis in CHO cells expressing hGR (IC50 = 41 nM), and in murine liver membranes. Orally active in vivo.

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Technical Data

M. Wt 467.79
Formula C24H20BrClN2O
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 191034-25-0
PubChem ID 5311276
Smiles CCCOC1=C(C=C(Br)C=C1)C1=C(NC(=C1)C1=CC=C(Cl)C=C1)C1=CC=NC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 46.78 100
ethanol 46.78 100

Preparing Stock Solutions

The following data is based on the product molecular weight 467.79. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.14 mL 10.69 mL 21.38 mL
5 mM 0.43 mL 2.14 mL 4.28 mL
10 mM 0.21 mL 1.07 mL 2.14 mL
50 mM 0.04 mL 0.21 mL 0.43 mL

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References are publications that support the biological activity of the product.

Cascieri et al (1999) Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor. J.Biol.Chem. 274 8694 PMID: 10085108

de Laszlo et al (1999) Potent, orally absorbed glucagon receptor antagonists. Bioorg.Med.Chem.Lett. 9 641 PMID: 10201821

Dallas-Yang et al (2001) Detection of glucagon-dependent GTPgS binding in high-throughput format. Anal.Biochem. 301 156

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