916170-19-9
916170-19-9 structure
- Name: AC-55541
- Chemical Name: AC 55541
- CAS Number: 916170-19-9
- Molecular Formula: C25H20BrN5O3
- Molecular Weight: 518.362
- Catalog: Signaling Pathways GPCR/G Protein Protease-Activated Receptor (PAR)
- Create Date: 2016-03-12 13:09:10
- Modify Date: 2024-01-09 15:27:28
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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.
| Name | AC 55541 |
|---|---|
| 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 |
| 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. |
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| Related Catalog | |
| References |
| 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℃ |