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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
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概述
LX7101 is a potent inhibitor of LIMK and ROCK2 with IC 50 values of 24, 1.6 and 10 nM for LIMK1 , LIMK2 and ROCK2 , respectively; also inhibits PKA with an IC 50 less than 1 nM.
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 IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:IC50: 24 nM (LIMK1), 1.6 nM (LIMK2), 10 nM (ROCK2), <1 nM (PKA)
规格
规格或纯度
10mM in DMSO
英文名称
LX7101
生化机理
LX7101 是 LIMK 和 ROCK2 的强效抑制剂，对 LIMK1、LIMK2 和 ROCK2 的 IC 50 值分别为 24、1.6 和 10 nM；对 PKA 也有抑制作用，IC 50 小于 1 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC1=CNC2=C1C(=NC=N2)N3CCC(CC3)(CN)C(=O)NC4=CC(=CC=C4)OC(=O)N(C)C
MeSH Entry Terms
LX-7101
分子量
451.52
高级数据
关联靶点（人）
ROCK2
Tclin
Rho 相关蛋白激酶 2(Rho-associated protein kinase 2)
(2 活性数据)
LIMK1
Tchem
LIM 结构域激酶 1(LIM domain kinase 1)
(2 活性数据)
LIMK2
Tchem
LIM 结构域激酶 2(LIM domain kinase 2)
(4 活性数据)
安全和危险性（GHS）
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 1192189-69-7，分子式为 C23H29N7O3，分子量为 451.52 g/mol。
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