L-161,982

Pricing Availability Delivery Time Qty
Cat.No. 2514 - L-161,982 | C32H29F3N4O4S2 | CAS No. 147776-06-5
Description: Selective EP4 receptor antagonist
Chemical Name: N-[[4'-[[3-Butyl-1,5-dihydro-5-oxo-1-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-4-yl]methyl][1,1'-biphenyl]-2-yl]sulfonyl]-3-methyl-2-thiophenecarboxamide
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Literature

Biological Activity

EP4 receptor antagonist that is selective over all other members of the prostanoid receptor family (Ki values are 0.024, 0.71, 1.90, 5.10, 5.63, 6.74, 19 and 23 μM for human EP4, TP, EP3, DP, FP, IP, EP1 and EP2 receptors respectively). Suppresses PGE2-induced bone formation in rats and prevents the nociceptive response induced by misoprostol in formalin-injected mice.

Compound Libraries

L-161,982 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 654.72
Formula C32H29F3N4O4S2
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 147776-06-5
PubChem ID 9961192
InChI Key MMDNKTXNUZFVKD-UHFFFAOYSA-N
Smiles CCCCC1=NN(C(=O)N1CC1=CC=C(C=C1)C1=C(C=CC=C1)S(=O)(=O)NC(=O)C1=C(C)C=CS1)C1=C(C=CC=C1)C(F)(F)F

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 65.47 100

Preparing Stock Solutions

The following data is based on the product molecular weight 654.72. 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 1.53 mL 7.64 mL 15.27 mL
5 mM 0.31 mL 1.53 mL 3.05 mL
10 mM 0.15 mL 0.76 mL 1.53 mL
50 mM 0.03 mL 0.15 mL 0.31 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

Certificate of Analysis / Product Datasheet
Select another batch:
Safety Datasheet

References

References are publications that support the products' biological activity.

Machwate et al (2001) Prostaglandin receptor EP4 mediates the bone anabolic effects of PGE2. Mol.Pharmacol. 60 36 PMID: 11408598

Oliva et al (2006) Role of periaqueductal grey prostaglandin receptors in formalin-induced hyperalgesia. Eur.J.Pharmacol. 530 40 PMID: 16360148

Balzary et al (2006) Lipopolysaccharide induces epithelium- and prostaglandin E2-dependent relaxation of mouse isolated trachea through activation of cyclooxygenase (COX)-1 and COX-2. J.Pharmacol.Exp.Ther. 317 806 PMID: 16464966


If you know of a relevant reference for L-161,982, please let us know.

View Related Products by Target

View Related Products by Product Action

View all Prostanoid Receptor Antagonists

Keywords: L-161,982, supplier, Selective, EP4, receptors, antagonists, Prostanoid, prostaglandins, prostacyclins, eicosanoids, L161982, Prostanoid, Receptors, Prostanoid, Receptors, Tocris Bioscience

1 Citation for L-161,982

Citations are publications that use Tocris products. Selected citations for L-161,982 include:

Chia et al (2011) Protection of protease-activated receptor 2 mediated vasodilatation against angiotensin II-induced vascular dysfunction in mice. BMC Pharmacol 11 10 PMID: 21955547


Do you know of a great paper that uses L-161,982 from Tocris? If so please let us know.

Reviews for L-161,982

There are currently no reviews for this product. Be the first to review L-161,982 and earn rewards!

Have you used L-161,982?

Submit a review and receive an Amazon gift card.

$10US/$10CAN/€7/£6 gift card for a review without an image

$25US/$25CAN/€18/£15 gift card for a review with an image

*Offer only valid in the USA / Canada, UK and Europe

Submit a Review

Literature in this Area

Cardiovascular

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

  • Hypertension
  • Thrombosis and Hemostasis
  • Atherosclerosis
  • Myocardial Infarction
  • Ischemia/Reperfusion Injury
  • Arrhythmias
  • Heart Failure
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
Immunology

Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

  • Chemokine and Cytokine Signaling
  • Chemotaxis
  • Complement System
  • Immune Cell Signaling
  • Inflammation
Asthma

Asthma Poster

Asthma is one of the most common chronic diseases in the world, affecting over 300 million people. This poster highlights key pathways and new therapies used to treat the condition, including those currently in clinical development.

Cardiovascular

Cardiovascular Poster

Cardiovascular disease remains one of the major causes of morbidity and mortality in the Western world and therefore this therapeutic area continues to be of great interest to researchers. This poster highlights the key GPCRs regulating vascular reactivity.

Pain

Pain Poster

Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.