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CAS No. : 1192189-69-7
MCE 国际站: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.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | Stem Cell Signaling Compound Library | TGF-beta/Smad Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Reprogramming Compound Library | Anti-COVID-19 Compound Library | Cytoskeleton Compound Library | Anti-Pulmonary Fibrosis Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | Chroman 1 dihydrochloride | Ripasudil free base | AS1892802 | Hu7691 free base | Sovesudil | AT13148 | CRT0066854 | Y-27632 dihydrochloride | RKI-1447 | HA-100 hydrochloride | WF-536 | Pentanoic acid-d9 | Fasudil dihydrochloride | ROCK-IN-5 | ROCK2-IN-5 | BDP5290 | PF-4950834 | PT-262 | Afuresertib hydrochloride | Belumosudil mesylate | GSK429286A | Y-27632 dihydrochloride (GMP) | H-1152 dihydrochloride | 3-(4-Pyridyl)indole | ROCK inhibitor-2 | ROCK-IN-7 | ZINC00881524
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货号: HY-12659
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