| Chemical Properties | Back Directory | [Boiling point ]
440.3±45.0 °C(Predicted) | [density ]
1.219±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
12.47±0.20(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pKi of 6.4 for hPAR2[1]. | [Biological Activity]
AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pKi of 6.4 for hPAR2[1].
AZ8838 binds in an occluded pocket[1].AZ8838 is a potent antagonist against SLIGRL-NH2 in the Ca2+ assay with a pIC50 of 5.70 ± 0.02[1].AZ8838 shows a potency trend when inhibiting IP1 production (pIC50 = 5.84 ± 0.02)[1].AZ8838 attenuates both peptide-induced phosphorylation of ERK1/2 (pIC50 = 5.7 ± 0.1) and β-arrestin-2 recruitment (pIC50 = 6.1 ± 0.1)[1].
AZ8838 (10 mg/kg; p.o.; 2 h prior) is anti-inflammatory in a PAR2 agonist-induced rat paw oedema model[1]. | [in vivo]
AZ8838 (10 mg/kg; p.o.; 2 h prior) is anti-inflammatory in a PAR2 agonist-induced rat paw oedema model[1]. | Animal Model: | Wistar rats, PAR2 agonist 2f-LIGRLO-NH2 induced acute oedema model[1] | | Dosage: | 10 mg/kg | | Administration: | Oral administration, once, 2?h prior | | Result: | Showed 60% reduction of paw swelling. Inhibited 2f-LIGRLO-NH2 induced activated mast cells, inhibited 2f-LIGRLO-NH2 decreased tryptase-positive (AA1+ve) intact mast cells in paw, blocked histamine release. |
| [IC 50]
PAR2 | [storage]
Store at -20°C | [References]
[1]. Kennedy AJ, et al. Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition. Commun Biol. 2020 Dec 17;3(1):782. |
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