详情描述
AC-55541 is a protease-activated receptor (PAR) 2 agonist. AC-55541activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 200 to 1000 nM. AC-55541 was well absorbed when administered intraperitoneally to rats, each reaching micromolar peak plasma concentrations. AC-55541 was stable to metabolism by liver microsomes and maintained sustained exposure in rats, with elimination half-lives of 6.1. Systemic administration of either AC-55541 or AC-264613 produced a similar degree of hyperalgesia as was observed when the compounds were administered locally. AC-55541 may be useful in probing the physiological functions of PAR2 receptors.
Product information
CAS Number: 916170-19-9
Molecular Weight: 518.36
Formula: C25H20BrN5O3
Chemical Name: (E)-N-(2-(2-(1-(3-bromophenyl)ethylidene)hydrazinyl)-2-oxo-1-(4-oxo-3,4-dihydrophthalazin-1-yl)ethyl)benzamide
Smiles: C/C(=N\NC(=O)C(NC(=O)C1C=CC=CC=1)C1=NNC(=O)C2=CC=CC=C21)/C1=CC(Br)=CC=C1
InChiKey: UCUHFWIFSHROPY-RWPZCVJISA-N
InChi: InChI=1S/C25H20BrN5O3/c1-15(17-10-7-11-18(26)14-17)28-31-25(34)22(27-23(32)16-8-3-2-4-9-16)21-19-12-5-6-13-20(19)24(33)30-29-21/h2-14,22H,1H3,(H,27,32)(H,30,33)(H,31,34)/b28-15+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: ≥ 51 mg/mL
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
References:
- Gardell LR, et al. Identification and characterization of novel small-molecule protease-activated receptor 2 agonists. J Pharmacol Exp Ther. 2008 Dec;327(3):799-808.
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