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LX7101

CAS No. : 1192189-69-7

MCE 站：LX7101

产品活性：LX7101是高效的LIMK和ROCK2抑制剂，对LIMK1/2, ROCK, PKA的IC₅₀分别为24，1.6，10，和小于1 nM。

研究领域：Cell Cycle/DNA Damage  |  Stem Cell/Wnt  |  Cytoskeleton  |  TGF-beta/Smad

作用靶点：ROCK

In Vitro: LX7101 is a dual LIM-kinase and ROCK inhibitor for the treatment of ocular hypertension and associated glaucoma. LX-7101 also displays potent inhibition of Akt1 with an IC₅₀ of less than 1 nM. The overall selectivity of LX7101 for LIMK2 increases at the higher physiological ATP concentrations. Under physiological conditions, the activity of LX7101 is primarily due to inhibition of LIMK2.

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

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