AZ8838

• CAT Number: I022814
• CAS Number: 2100285-41-2
• Molecular Formula: C13H15FN2O
• Molecular Weight: 234.27
• Purity: ≥95%
• Synonyms: (S)-(4-fluoro-2-propylphenyl)-(1H-imidazol-2-yl)methanol
• InChI: InChI=1S/C13H15FN2O/c1-2-3-9-8-10(14)4-5-11(9)12(17)13-15-6-7-16-13/h4-8,12,17H,2-3H2,1H3,(H,15,16)/t12-/m0/s1
• InChIKey: IDFPQEHZYBXIFO-LBPRGKRZSA-N
• SMILES: CCCC1=C(C=CC(=C1)F)C(C2=NC=CN2)O

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].

Reference

[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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