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PAR-2 Agonist III
(E)-N-((1-(3-Bromophenyl)-ethylidene-hydrazinocarbonyl)-(4-oxo-3,4-dihydro-phthalazin-1-yl)-methyl)-benzamide, AC-55541
This product has been discontinued.
A cell-permeable, nonpeptidic phthalazinyl-hydrazide compound that induces cellular proliferation, PI hydrolysis, and Ca2+ mobilization (pEC50 = 6.7, 5.9, 6.6, in PAR-2-expressing NIH3T3, HEK 293T, and KNRK cultures, respectively) in a PAR-2-, but not PAR-1/3/4-, dependent manner, while exhibiting no significant affinity toward a panel of over 30 other receptors and channels implicated in nociception and inflammation. Shown to effectively elicit edema (by ~18%, 4 h after a direct injection dose of 30 ng/paw) and increased thermal hyperalgesia (by ~24% and ~85% drop in response time, respectively, 2 h after a direct injection dose of 30 ng/paw or an i.p. dose of 10 mg/kg) in rat models of acute inflammation and nociception in vivo. AC-55541 is metabolically stable (6 and 19 µl/min/mg, respectively, in human and rat liver microsome preparations) and pharmacokinetic studies reveal a peak plasma concentration of 1035 ng/ml at 50 min after an i.p. dose of 10 mg/kg and an elimination half-life of 6.1 h in rats in vivo.
产品信息
Form White solid
Molar mass 518.4
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥95% by HPLC
Solubility DMSO
Chemical formula C25H20BrN5O3
CAS number 916170-19-9
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling |