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AC 55541

Catalog No.GC15290

AC 55541은 고도로 선택적인 프로테아제 활성화 수용체 2(PAR2) 작용제(pEC50\u003d6.7)로, 다른 PAR 하위 유형이나 통각 및 염증과 관련된 30개 이상의 다른 수용체에서 활성을 나타내지 않습니다.

Products are for research use only. Not for human use. We do not sell to patients.

AC 55541 Chemical Structure

Cas No.: 916170-19-9

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10mg
US$119.00
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50mg
US$483.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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].

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.

Chemical Properties

Cas No. 916170-19-9 SDF
Chemical Name (E)-N-(2-(2-(1-(3-bromophenyl)ethylidene)hydrazinyl)-2-oxo-1-(4-oxo-3,4-dihydrophthalazin-1-yl)ethyl)benzamide
Canonical SMILES O=C1C2=CC=CC=C2C(C(NC(C3=CC=CC=C3)=O)C(N/N=C(C)/C4=CC=CC(Br)=C4)=O)=NN1
Formula C25H20BrN5O3 M.Wt 518.36
Solubility DMF: 15 mg/ml,DMF:PBS (pH 7.2) (1:8): 0.11 mg/ml,DMSO: 10 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.9292 mL 9.6458 mL 19.2916 mL
5 mM 0.3858 mL 1.9292 mL 3.8583 mL
10 mM 0.1929 mL 0.9646 mL 1.9292 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 13 reference(s) in Google Scholar.)

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