AZ-8838 manufacturers
- AZ8838
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- $1128.00 / 25mg
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2025-10-27
- CAS:2100285-41-2
- Min. Order:
- Purity:
- Supply Ability: 10g
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| | AZ-8838 Basic information |
| Product Name: | AZ-8838 | | Synonyms: | AZ-8838;(R)-(4-Fluoro-2-propylphenyl)(1H-imidazol-2- yl)methanol;1H-Imidazole-2-methanol, α-(4-fluoro-2-propylphenyl)-, (αS)-;(S)-(4-Fluoro-2-propylphenyl)(1H-imidazol-2-yl)methanol | | CAS: | 2100285-41-2 | | MF: | C13H15FN2O | | MW: | 234.27 | | EINECS: | | | Product Categories: | | | Mol File: | 2100285-41-2.mol |  |
| | AZ-8838 Chemical Properties |
| Boiling point | 440.3±45.0 °C(Predicted) | | density | 1.219±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | pka | 12.47±0.20(Predicted) | | form | Solid | | color | Off-white to light yellow |
| | AZ-8838 Usage And Synthesis |
| 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 | | 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. |
| | AZ-8838 Preparation Products And Raw materials |
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