AC-55541

Modify Date: 2025-08-23 07:31:49

AC-55541 Structure
AC-55541 structure
Common Name AC-55541
CAS Number 916170-19-9 Molecular Weight 518.362
Density 1.5±0.1 g/cm3 Boiling Point N/A
Molecular Formula C25H20BrN5O3 Melting Point N/A
MSDS Chinese USA Flash Point N/A

 Use of AC-55541


AC-55541 is a novel small-molecule protease-activated receptor 2(PAR2) agonist; activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 200 to 1000 nM.IC50 value: 200-1000 nM(EC50) [1]Target: PAR2 agonistNeither AC-55541 nor AC-264613 had activity at any of the other PAR receptor subtypes, nor did they have any significant affinity for over 30 other molecular targets involved in nociception. Visualization of EYFP-tagged PAR2 receptors showed that each compound stimulated internalization of PAR2 receptors. AC-55541 was well absorbed when administered intraperitoneally to rats, 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 h. Intrapaw administration of AC-55541 or AC-264613 elicited robust and persistent thermal hyperalgesia and edema. Coadministration of either a tachykinin 1 (neurokinin 1) receptor antagonist or a transient receptor potential vanilloid (TRPV) 1 antagonist completely blocked these effects. Systemic administration of either AC-55541 or AC-264613 produced a similar degree of hyperalgesia as was observed when the compounds were administered locally.

 Names

Name AC 55541
Synonym More Synonyms

 AC-55541 Biological Activity

Description AC-55541 is a novel small-molecule protease-activated receptor 2(PAR2) agonist; activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 200 to 1000 nM.IC50 value: 200-1000 nM(EC50) [1]Target: PAR2 agonistNeither AC-55541 nor AC-264613 had activity at any of the other PAR receptor subtypes, nor did they have any significant affinity for over 30 other molecular targets involved in nociception. Visualization of EYFP-tagged PAR2 receptors showed that each compound stimulated internalization of PAR2 receptors. AC-55541 was well absorbed when administered intraperitoneally to rats, 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 h. Intrapaw administration of AC-55541 or AC-264613 elicited robust and persistent thermal hyperalgesia and edema. Coadministration of either a tachykinin 1 (neurokinin 1) receptor antagonist or a transient receptor potential vanilloid (TRPV) 1 antagonist completely blocked these effects. Systemic administration of either AC-55541 or AC-264613 produced a similar degree of hyperalgesia as was observed when the compounds were administered locally.
Related Catalog
References

[1]. 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.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Molecular Formula C25H20BrN5O3
Molecular Weight 518.362
Exact Mass 517.074951
PSA 116.31000
LogP 4.65
Index of Refraction 1.689
Storage condition -20℃

 Synonyms

N-[2-{(2E)-2-[1-(3-Bromophenyl)ethylidene]hydrazino}-2-oxo-1-(4-oxo-3,4-dihydro-1-phthalazinyl)ethyl]benzamide
1-Phthalazineacetic acid, α-(benzoylamino)-3,4-dihydro-4-oxo-, 2-[(1E)-1-(3-bromophenyl)ethylidene]hydrazide
N-[2-{(2E)-2-[1-(3-Bromophenyl)ethylidene]hydrazino}-2-oxo-1-(4-oxo-3,4-dihydrophthalazin-1-yl)ethyl]benzamide
(2E)-2-[1-(3-Bromophenyl)ethylidene]α-(benzoylamino)-3,4-dihydro-4-oxo-1-phthalazineaceticacidhydrazide
AC-55541
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