Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZ8838 is an effective, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pK i of 6.4 for hPAR2 [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,270.00 | |
50 mg | 6-8 weeks | $ 1,650.00 | |
100 mg | 6-8 weeks | $ 2,650.00 |
Description | AZ8838 is an effective, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pK i of 6.4 for hPAR2 [1]. |
In vitro | AZ8838 demonstrates potent antagonistic activity by binding to an occluded pocket, significantly inhibiting SLIGRL-NH2 in Ca2+ assays with a pIC50 of 5.70 ± 0.02. It also shows a consistent potency trend in reducing IP1 production (pIC50 = 5.84 ± 0.02) and effectively attenuates peptide-induced phosphorylation of ERK1/2 (pIC50 = 5.7 ± 0.1) alongside β-arrestin-2 recruitment (pIC50 = 6.1 ± 0.1). |
In vivo | AZ8838 (10 mg/kg; p.o.; 2 h prior) demonstrated anti-inflammatory effects in a rat paw oedema model induced by the PAR2 agonist 2f-LIGRLO-NH2 [1]. Utilizing Wistar rats in an acute oedema model, a single oral dose was administered 2 hours before induction, resulting in a 60% reduction in paw swelling. The compound effectively inhibited the activation of mast cells induced by 2f-LIGRLO-NH2, reduced the number of tryptase-positive (AA1+ve) intact mast cells in the paw, and blocked histamine release. |
Molecular Weight | 234.27 |
Formula | C13H15FN2O |
CAS No. | 2100285-41-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
AZ8838 2100285-41-2 inhibitor inhibit