PAR2 Antagonist

AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC₅₀ of 23 nM.

AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pK_i of 6.4 for hPAR2.

I-191 is a potent, selective protease-activated receptor 2 (PAR2) antagonist.

ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 hydrochloride reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 hydrochloride also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 hydrochloride can be used in the study of endometriosis and liver fibrosis.

GB83 is a potent PAR2 antagonist. GB83 reverses neutrophil elastase‐induced synovitis and pain. GB83 blocks the effect of MET-1 supernatant on NG neurons.

ENMD-1068 is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 can be used in the study of endometriosis and liver fibrosis.

K-14585 is a peptide competitive PAR2 antagonist. K-14585 inhibits PAR2-dependent IL-8 production, NF-κB phosphorylation, and p38 signaling. K-14585 reduces SLIGKV (PAR2 agonist peptide)-induced Ca²⁺ mobilisation in primary human keratinocytes.

(R)-AZ8838 is a competitive PAR2 antagonist with a pK_i of  5.2 for human PAR2. (R)-AZ8838 exert anti-inflammatory effects in a rat model of PAR2 agonist-induced paw oedema.

ENMD-1068 hydrobromide is a potent PAR2 antagonist. ENMD-1068 hydrobromide attenuates joint inflammation in a dose-dependent manner. ENMD-1068 hydrobromide can be used in research of joint inflammation.