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LX7101
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LX7101图片
CAS NO:1192189-69-7
包装与价格:
包装价格(元)
5 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
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。

产品描述

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).

体外活性

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.

体内活性

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].

Cas No.

1192189-69-7

分子式

C23H29N7O3

分子量

451.52

储存和溶解度

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