LX7101是LIMK和ROCK2高效抑制剂，对LIMK1/2、ROCK、PKA的IC50分别为24、1.6、10 和小于1 nM。

LX7101 is an effective inhibitor of LIMK and ROCK2 (IC50: 24, 1.6, and 10 nM for LIMK1, LIMK2, and ROCK2, respectively). It also inhibits PKA (IC50<1 nM).

LX7101 is a dual LIM-kinase and ROCK inhibitor for the treatment of ocular hypertension and associated glaucoma. LX-7101 also shows effective inhibition of Akt1 (IC50<1 nM)[1]. The activity of LX7101 is primarily due to inhibition of LIMK2, under physiological conditions[2]. The overall selectivity of LX7101 for LIMK2 enhances the higher physiological ATP concentrations.

Topical doses of LX-7101 are evaluated for tolerability in the eyes of mice, rats, and rabbits. It is well tolerated at doses up to 0.5% in non-GLP single-dose studies. LX-7101 is advanced to Phase-I clinical trials as intraocular pressure (IOP)-lowering agent for the treatment of glaucoma. LX-7101 shows a significant IOP reduction at time points ranging from 1 h to 6 h post-administration in rabbits[1]. LX-7101 (5%) achieved an additional reduction of IOP (5.0 mmHg total reduction) compared to the 0.1% formulation. It also demonstrated a long duration of action, in the mouse IOP assay, with IOP not returning to baseline until more than 8 h postdose[2].

1192189-69-7

C23H29N7O3

451.52

DMSO:150 mg/mL (332.21 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years