AC 55541, protease-activated receptor 2 (PAR2) agonist (ab218603)

Overview

  • Product name

    AC 55541, protease-activated receptor 2 (PAR2) agonist
  • Description

    Potent, selective protease-activated receptor 2 (PAR2) agonist
  • Alternative names

    • AC-55541
    • AC55541
    • N-[[1-(3-bromo-phenyl)-eth-(E)-ylidene-hydrazinocarbonyl]-(4-oxo-3,4-dihydro-phthalazin-1-yl)-methyl]-benzamide
  • Biological description

    Potent, selective protease-activated receptor 2 (PAR2) agonist that displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation. Stimulates cell proliferation, PI hydrolysis and Ca2+ mobilization in vitro (pEC50 values are 6.7, 5.9 and 6.6 respectively) and exhibits pronociceptive activity in vivo.

  • Purity

    > 98%
  • CAS Number

    916170-19-9
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    (2E)-2-[1-(3-Bromophenyl)ethylidene] α-(benzoylamino)-3,4-dihydro-4-oxo-1-phthalazineacetic acid hydrazide
  • Molecular weight

    518.36
  • Molecular formula

    C25H20BrN5O3
  • PubChem identifier

    9589606
  • Storage instructions

    Shipped at 4°C. Store at -20°C. Store In the Dark. Store under desiccating conditions.
  • Solubility overview

    Soluble in DMSO to 50 mM
  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    C/C(=N\NC(=O)C(C1=NNC(=O)C2=CC=CC=C21)NC(=O)C3=CC=CC=C3)/C4=CC(=CC=C4)Br
  • Source

    Synthetic

References

This product has been referenced in:

  • Tripathi T  et al. Protease-activated receptor 2 (PAR2) is upregulated by Acanthamoeba plasminogen activator (aPA) and induces proinflammatory cytokine in human corneal epithelial cells. Invest Ophthalmol Vis Sci 55:3912-21 (2014). Read more (PubMed: 24876278) »
  • Ma JN & Burstein ES The protease activated receptor 2 (PAR2) polymorphic variant F240S constitutively activates PAR2 receptors and potentiates responses to small-molecule PAR2 agonists. J Pharmacol Exp Ther 347:697-704 (2013). Read more (PubMed: 24078870) »
  • Seitzberg JG  et al. Discovery of potent and selective small-molecule PAR-2 agonists. J Med Chem 51:5490-3 (2008). Read more (PubMed: 18720984) »
  • Gardell LR  et al. Identification and characterization of novel small-molecule protease-activated receptor 2 agonists. J Pharmacol Exp Ther 327:799-808 (2008). Read more (PubMed: 18768780) »

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Please note: All products are "FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC PROCEDURES, NOT FOR USE IN HUMANS"
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