AC 55541 |
| رقم الكتالوجGC15290 |
AC 55541 هو ناهض للمستقبل 2 (PAR2) الذي ينشط البروتياز انتقائيًا للغاية (pEC50 \u003d 6.7) ، ولا يظهر أي نشاط في الأنواع الفرعية الأخرى من PAR أو في أكثر من 30 مستقبلًا آخر متورط في الشعور بالألم والالتهاب.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 916170-19-9
Sample solution is provided at 25 µL, 10mM.
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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.
| 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 |
| الذوبان | 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. | ||
| Prepare stock solution | |||
|
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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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)
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