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LX7101 HCL
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 HCL图片
CAS NO:1192189-69-7
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
2mg电议
5mg电议
10mg电议
50mg电议

产品介绍
LX7101 HCL 是一种有效的 LIMK 和 ROCK2 抑制剂,对 LIMK1、LIMK2 和 ROCK2 的 IC50 值分别为 24、1.6 和 10 nM;还抑制 PKA,IC50 小于 1 nM。
Cas No.1192189-69-7
化学名InChI=1S/C23H29N7O3.ClH/c1-15-12-25-19-18(15)20(27-14-26-19)30-9-7-23(13-24,8-10-30)21(31)28-16-5-4-6-17(11-16)33-22(32)29(2)3;/h4-6,11-12,14H,7-10,13,24H2,1-3H3,(H,28,31)(H,25,26,27);1H
Canonical SMILESCC1=CNC2=NC=NC(N3CCC(C(NC4=CC(OC(N(C)C)=O)=CC=C4)=O)(CN)CC3)=C21.Cl
分子式C23H30ClN7O3
分子量487.98
溶解度<4.88mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Description:

IC50: 4.3, 32, 69 and 32 nM for LIMK2, KIMK1, ROCK1 and ROCK2, respectivley

LIM-kinases 1 and 2 (LIMK1 and LIMK2) regulate cytoskeletal dynamics by phosphorylating and deactivating cofilin, a protein that depolymerizes actin filaments. ROCK, a kinase upstream of LIMK in the signaling cascade that regulates actin filament dynamics, are being investigated in the clinic for reduction of IOP through relaxation of the trabecular meshwork. LX7101 is a dual LIM-kinase and ROCK inhibitor for the treatment of glaucoma.

In vitro: LX7101 proved significantly more selective for LIMK2. In addition, LX7101 was screened against a panel of 403 kinases. Moderate selectivity was observed in this screen (34 assays including LIMK2 and ROCK2 indicated that the Kd is most likely<1 μM) [1].

In vivo: At a well-tolerated dose, LX7101 achieved additional reduction of IOP 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. More critically, LX7101 produced a significantly greater reduction of IOP than either timolol or latanoprost [1].

Clinical trial: LX7101 completed IND enabling studies and was tested in a Phase 1 clinical trial in glaucoma patients, where it showed efficacy in lowering intraocular pressure [1].

Reference:
[1] Harrison BA, Almstead ZY, Burgoon H, Gardyan M, Goodwin NC, Healy J, Liu Y, Mabon R, Marinelli B, Samala L, Zhang Y, Stouch TR, Whitlock NA, Gopinathan S, McKnight B, Wang S, Patel N, Wilson AG, Hamman BD, Rice DS, Rawlins DB.  Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma. ACS Med Chem Lett. 2014 Nov 24;6(1):84-8.