AC-55541
AC-55541 Basic information
- Product Name:
- AC-55541
- Synonyms:
-
- (2E)-2-[1-(3-Bromophenyl)ethylidene]α-(benzoylamino)-3,4-dihydro-4-oxo-1-phthalazineaceticacidhydrazide
- AC 55541
- CS-2020
- CS-1802
- AC 55541,(2E)-2-[1-(3-Bromophenyl)ethylidene]α-(benzoylamino)-3,4-dihydro-4-oxo-1-phthalazineaceticacidhydrazide
- (E)-N-(2-(2-(1-(3-Bromophenyl)ethylidene)hydrazinyl)-2-oxo-1-(4-oxo-3,4-dihydrophthalazin-1-yl)ethyl)benzamide
- AC55541; AC-55541
- (2E)-2-[1-(3-Bromophenyl)ethylidene] α-(benzoylamino)-3,4-dihydro-4-oxo-1-phthalazineacetic acid hydrazide AC55541
- CAS:
- 916170-19-9
- MF:
- C25H20BrN5O3
- MW:
- 518.36
- EINECS:
- 604-604-1
- Product Categories:
-
- Inhibitors
- Mol File:
- 916170-19-9.mol
AC-55541 Chemical Properties
- Density
- 1.49±0.1 g/cm3(Predicted)
- storage temp.
- Inert atmosphere,Store in freezer, under -20°C
- solubility
- Soluble in DMSO
- form
- powder
- pka
- 10.99±0.46(Predicted)
- color
- White to off-white
AC-55541 Usage And Synthesis
Uses
AC 55541 is a selective protease-activated receptor 2 agonist.
Definition
ChEBI: AC-55541 is an organic molecular entity.
Biological Activity
ac 55541 is a potent agonist of par2 with pec50 value of 6.7 and functions range from 200 to 1000 nm [1-3].protease-activated receptor 2 (par2) is a member of the large family of 7-transmembrane receptors and plays an important role in modulating inflammatory responses and acting as a sensor for proteolytic enzymes generated during infection [2].ac 55541 is a selective par2 agonist and has no effect on par1. using a cellular proliferation assay (r-sat), it showed that ac 55541 stimulated nih-3t3 cells proliferation by activating par2 and receptor with f240s mutation constitutively active in all functional assays which nearly 30-fold sensitive to ac 55541 than sligrl and 2-furorl ligrlo [1, 2]. when tested with human corneal epithelial (hce) cells, administration of ac 55541 significantly induced the expression of par2 and inhibited acanthamoeba plasminogen activator (apa) [3].in male sprague-dawley rat model with acute thermal nociception and edema in paw induced by sligrl-nh2 or trypsin, intrapaw administration of ac 55541 induced hind paw edema and thermal hyperalgesia at the doses as low as 30 ng and showed dose-dependent pronociceptive effects [1].
IC 50
PAR2
storage
Store at -20°C
References
1. gardell, l.r., et al., identification and characterization of novel small-molecule protease-activated receptor 2 agonists. j pharmacol exp ther, 2008. 327(3): p. 799-808.2. ma, j.n. and e.s. burstein, the protease activated receptor 2 (par2) polymorphic variant f240s constitutively activates par2 receptors and potentiates responses to small-molecule par2 agonists. j pharmacol exp ther, 2013. 347(3): p. 697-704.3. tripathi, t., m. abdi, and h. alizadeh, 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, 2014. 55(6): p. 3912-21.
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