AC 264613 |
| رقم الكتالوجGC14831 |
AC 264613 هو ناهض قوي وانتقائي لمستقبلات البروتياز (PAR-2) مع pEC50 من 7.5.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1051487-82-1
Sample solution is provided at 25 µL, 10mM.
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AC 264613 is a potent agonist of PAR2 with pEC50 value of 7.5 and potencies range from 30 to 100 nM [1, 2].
Protease-activated receptor 2 (PAR2) also known as coagulation factor II (thrombin) receptor-like 1 (F2RL1) or G-protein coupled receptor 11 (GPR11) is expressed in vascular tissue and highly vascular organs and involves in the vascular tone regulation. It has been shown that PAR2 plays a pivotal role in vessel inflammation and wound healing processes [2].
AC 264613 is a selective PAR2 agonist and has no effect on other PARs. When tested with HEK 293 T cells (PAR2 wild type) and KNRK cells (transfected with human PAR2 receptors) for stimulates PI hydrolysis and Ca2+ mobilization assays, AC 264613 showed effect with pEC50 value of 6.9 and 7.0,respectively [1]. Using QuickChange Mutagenesis manner, NIH 3T3 cells were made with ECL2 mutations in Q233E, E232R, E232R/Q233R, F240S, and F240S/S37P receptors and AC 264613 treatment PAR2 F240S receptors were constitutively expressed in multiple functional endpoints while had no effect on E232 and Q233 mutaions [2].
In male Sprague-Dawley rat model with acute thermal nociception and edema in paw induced by SLIGRL-NH2 or trypsin, intrapaw administration of AC 264613 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.
| Cas No. | 1051487-82-1 | SDF | |
| Chemical Name | (3S,4R)-N-[(Z)-1-(3-bromophenyl)ethylideneamino]-2-oxo-4-phenylpyrrolidine-3-carboxamide | ||
| Canonical SMILES | CC(=NNC(=O)C1C(CNC1=O)C2=CC=CC=C2)C3=CC(=CC=C3)Br | ||
| Formula | C19H18BrN3O2 | M.Wt | 400.27 |
| الذوبان | <40.03mg/ml in DMSO | 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 | 2.4983 mL | 12.4916 mL | 24.9831 mL |
| 5 mM | 0.4997 mL | 2.4983 mL | 4.9966 mL |
| 10 mM | 0.2498 mL | 1.2492 mL | 2.4983 mL |
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- Purity: >95.00%
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