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Submit ReviewAC 55541
Description: Potent and selective PAR2 agonist
Chemical Name: (2E)-2-[1-(3-Bromophenyl)ethylidene] α-(benzoylamino)-3,4-dihydro-4-oxo-1-phthalazineacetic acid hydrazide
Purity: ≥97% (HPLC)
Biological Activity for AC 55541
AC 55541 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 6.7) 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.
Technical Data for AC 55541
| M. Wt | 518.36 |
| Formula | C25H20BrN5O3 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 916170-19-9 |
| PubChem ID | 9589606 |
| InChI Key | UCUHFWIFSHROPY-RWPZCVJISA-N |
| Smiles | O=C2C1=CC=CC=C1C(C(NC(C3=CC=CC=C3)=O)C(N/N=C(C)/C4=CC=CC(Br)=C4)=O)=NN2 |
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 Data for AC 55541
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 25.92 | 50 |
Preparing Stock Solutions for AC 55541
The following data is based on the product molecular weight 518.36. 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 |
|---|---|---|---|
| 0.5 mM | 3.86 mL | 19.29 mL | 38.58 mL |
| 2.5 mM | 0.77 mL | 3.86 mL | 7.72 mL |
| 5 mM | 0.39 mL | 1.93 mL | 3.86 mL |
| 25 mM | 0.08 mL | 0.39 mL | 0.77 mL |
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Product Datasheets for AC 55541
References for AC 55541
References are publications that support the biological activity of the product.
Seitzberg et al (2008) Discovery of potent and selective small-molecule PAR-2 agonists. J.Med.Chem. 51 5490 PMID: 18720984
Gardell et al (2008) Identification and characterization of novel small-molecule protease-activated receptor 2 agonists. J.Pharmacol.Exp.Ther. 327 799 PMID: 18768780
If you know of a relevant reference for AC 55541, please let us know.
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Keywords: AC 55541, AC 55541 supplier, Potent, selective, PAR2, agonists, Receptors, Protease-Activated, proteinase-activated, AC55541, 3369, Tocris Bioscience
6 Citations for AC 55541
Citations are publications that use Tocris products. Selected citations for AC 55541 include:
Shi et al (2015) Alterations in serotonin, transient receptor potential channels and protease-activated receptors in rats with irritable bowel syndrome attenuated by Shugan decoction. J Immunol 21 4852 PMID: 25944998
White et al (2015) A brief exposure to tryptase or thrombin potentiates fibrocyte differentiation in the presence of serum or serum amyloid p. Mol Pain 194 142 PMID: 25429068
Tripathi et al (2014) 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 PMID: 24876278
Alkhani et al (2014) Contribution of TRPC3 to store-operated calcium entry and inflammatory transductions in primary nociceptors. Neuropsychopharmacology 10 43 PMID: 24965271
Shi et al (2019) Identification and therapeutic rescue of autophagosome and glutamate receptor defects in C9ORF72 and sporadic ALS neurons. JCI Insight 5 PMID: 31310593
Melo et al (2019) Exosome-mediated uptake of mast cell tryptase into the nucleus of melanoma cells: a novel axis for regulating tumor cell proliferation and gene expression. Cell Death Dis 10 659 PMID: 31506436
Do you know of a great paper that uses AC 55541 from Tocris? Please let us know.
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