L-168,049

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

Catalog # 2311 | Tocris Bioscience a Bio-Techne Brand

Citations (1)

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:	≥99% (HPLC)
Molecular Weight:	467.79

View Full Technical Details for L-168,049

Technical Data
Citations (1) / Reviews

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	≥99% (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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt*

g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1 (C1)

Volume 1 (V1)

Concentration 2 (C2)

Volume 2 (V2)

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

References for L-168,049

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

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
de Laszlo Potent, orally absorbed glucagon receptor antagonists. Bioorg.Med.Chem.Lett. 1999 PMID: 10201821

Citations for L-168,049 (1)

Showing 1 - 1 of 1 citation Showing All

Search Title:

Citations are publications that use Bio-Techne products. Selected citations for L-168,049 include:

Rodriguez-Diaz et al. (2018) Paracrine Interactions within the Pancreatic Islet Determine the Glycemic Set Point. Cell Metab. 27:549
PMID: 29514065

There are no citations that match your criteria.