L-168,049

Name: L-168,049
Brand: Tocris Bioscience
SKU: 2311

Tocris Bioscience, part of Bio-Techne | Catalog # 2311

Citations (12)

COA / SDS

Potent, orally active human glucagon receptor antagonist

Key Product Details

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:	≥98% (HPLC)
Molecular Weight:	467.79

View Full Technical Details for L-168,049

Technical Data
Citations

Biological Activity for L-168,049

L-168,049 is a 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.

Compound Libraries for L-168,049

L-168,049 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for L-168,049

M. Wt	467.79
Formula	C₂₄H₂₀BrClN₂O
Storage	Store at RT
Purity	≥98% (HPLC)
CAS Number	191034-25-0
PubChem ID	5311276
InChi Key	HHBOWXZOLYQFNY-UHFFFAOYSA-N
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 for L-168,049

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

Preparing Stock Solutions for L-168,049

The following data is based on the product molecular weight 467.79.

Batch specific molecular weights may vary from batch to batch due to the degree 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 for L-168,049

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

de Laszlo Potent, orally absorbed glucagon receptor antagonists. Bioorg.Med.Chem.Lett. 1999 PMID: 10201821
Dallas-Yang Detection of glucagon-dependent GTPgS binding in high-throughput format. Anal.Biochem.
Cascieri Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor. J.Biol.Chem. 1999 PMID: 10085108