AZ-8838
- Product Name
- AZ-8838
- CAS No.
- 2100285-41-2
- Chemical 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)-
- CBNumber
- CB34667587
- Molecular Formula
- C13H15FN2O
- Formula Weight
- 234.27
- MOL File
- 2100285-41-2.mol
AZ-8838 Property
- 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 Chemical Properties,Usage,Production
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].
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
Raw materials
Preparation Products
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