L-168,049

Pricing Availability Delivery Time Qty
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)
Datasheet
Citations
Literature

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.

Compound Libraries

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

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
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.

Select a batch to recalculate based on the batch molecular weight:
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.
=
x
x
g/mol

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

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.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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 PMID:


If you know of a relevant reference for L-168,049, please let us know.

View Related Products by Target

View Related Products by Product Action

View all Glucagon Receptor Antagonists

Keywords: L-168,049, supplier, Potent, orally, active, human, glucagon, receptor, antagonists, Receptors, L168049, Glucagon, Receptor, Tocris Bioscience

Citations for L-168,049

Citations are publications that use Tocris products.

Currently there are no citations for L-168,049. Do you know of a great paper that uses L-168,049 from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Peptide Hormone Receptors

Peptide Hormone Receptors Product Listing

A collection of over 200 products for peptide hormone receptors, the listing includes research tools for the study of:

  • Anterior Pituitary Regulation
  • Blood Pressure Regulation
  • Feeding and Appetite Regulation
  • Glucose Regulation
  • Peptide Hormone Processing
Peptides Involved in Appetite Modulation

Peptides Involved in Appetite Modulation Scientific Review

Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.

Pathways for L-168,049

Protocols

TODO: Add Protocols