PAR2 modulator-1 is a biased protease-activated receptor 2 ( PAR2 ) inhibitor. PAR2 modulator-1 blocks the PAR2 -dependent MAPK signaling pathway with an IC50 value of 8.5 μM, without altering the PAR2 -dependent Ca 2+ signaling pathway. PAR2 modulator-1 blocks pain responses induced by PAR2 agonists. PAR2 modulator-1 can be used in the research of chronic pain [1].
In Vivo, PAR2 modulator-1 (C781) (1 μg; intraplantar injection; single dose) effectively blocks 2AT-induced persistent mechanical hyperalgesia without inducing pain on its own[1]. PAR2 modulator-1 (30 mg/kg; i.p.; single dose) effectively blocks 2AT-induced systemic mechanical hyperalgesia.
In Vitro, PAR2 modulator-1 (C781) (30-300 nM) inhibits 2AT-induced PAR2 responses in a dose-dependent manner, with almost complete inhibition observed at 300 nM[1]. PAR2 modulator-1 (100 nM-100 μM) significantly reduces MAPK phosphorylation in cells expressing PAR2, with an IC50 of 8.5 μM[1].
References:
[1]. Scott A. BOITANO, et al. Small molecule modulators of par2 and uses thereof. WO2019199800A1. 2020-10-09
In Vivo, PAR2 modulator-1 (C781) (1 μg; intraplantar injection; single dose) effectively blocks 2AT-induced persistent mechanical hyperalgesia without inducing pain on its own[1]. PAR2 modulator-1 (30 mg/kg; i.p.; single dose) effectively blocks 2AT-induced systemic mechanical hyperalgesia.
In Vitro, PAR2 modulator-1 (C781) (30-300 nM) inhibits 2AT-induced PAR2 responses in a dose-dependent manner, with almost complete inhibition observed at 300 nM[1]. PAR2 modulator-1 (100 nM-100 μM) significantly reduces MAPK phosphorylation in cells expressing PAR2, with an IC50 of 8.5 μM[1].
References:
[1]. Scott A. BOITANO, et al. Small molecule modulators of par2 and uses thereof. WO2019199800A1. 2020-10-09