| 产品编号 |
产品名称 |
产品包装 |
产品价格 |
| SC6542-5mg |
K-115 (ROCK抑制剂) |
5mg |
1067.00元 |
化学信息：
|
化学名
|
4-fluoro-5-[[(2S)-2-methyl-1,4-diazepan-1-yl]sulfonyl]isoquinoline
|
|
|
简称
|
K-115
|
|
别名
|
K115 compound, Glanatec, Ripasudil
|
|
中文名
|
N/A
|
|
化学式
|
C15H18FN3O2S
|
|
分子量
|
323.39
|
|
CAS号
|
223645-67-8
|
|
纯度
|
98%
|
|
溶剂/溶解度
|
Water<1mg/ml; DMSO4mg/ml; Ethanol<1mg/ml
|
|
溶液配制
|
5mg加入1.55ml DMSO，或者每3.23mg加入1ml DMSO，配制成10mM溶液。SC6542-10mM用DMSO配制。
|
生物信息：
|
产品描述
|
K-115, an isoquinolinesulfonamide compound, is a highly selective and potent (IC50=31nM) Rho-kinase inhibitor; is in Phase II clinical development in patients with POAG or ocular hypertension.
|
|
信号通路
|
Cell Cycle; DNA Damage
|
|
靶点
|
ROCK
|
－
|
－
|
－
|
－
|
|
IC50
|
31nM
|
－
|
－
|
－
|
－
|
|
体外研究
|
K-115 had selective and potent inhibitory effects on ROCKs. In rabbits, topical instillation of K-115 significantly reduced IOP in a dose-dependent manner. Maximum IOP reduction was observed 1h after topical instillation, which was 8.55±1.09mmHg (mean±SE) from the baseline IOP at 0.5%. In monkeys, maximum IOP reduction was observed 2h after topical instillation, which was 4.36±0.32mmHg from the baseline IOP at 0.4%, and was significantly stronger than that of 0.005% latanoprost. Whole-head autoradiography showed that the radioactivity level was maximum at 15min after instillation of [(14)C]K-115 in the ipsilateral eye.
NC-induced oxidative stress, including oxidation of lipids and production of ROS, was significantly attenuated by K-115. Furthermore, expression of the Nox gene family, especially Nox1, which is involved in the NC-induced ROS production pathway, was dramatically reduced by K-115.
|
|
体内研究
|
N/A
|
|
临床实验
|
N/A
|
|
特征
|
N/A
|
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
|
酶活性检测实验
|
|
方法
|
N/A
|
|
细胞实验
|
|
细胞系
|
N/A
|
|
浓度
|
N/A
|
|
处理时间
|
N/A
|
|
方法
|
N/A
|
|
动物实验
|
|
动物模型
|
N/A
|
|
配制
|
N/A
|
|
剂量
|
N/A
|
|
给药方式
|
N/A
|
参考文献：
1. Tanihara H, et al. JAMA Ophthalmol. 2013 Oct, 131(10), 1288-95.
2. Isobe T, et al. Curr Eye Res. 2014 Aug, 39(8), 813-22.
包装清单：
|
产品编号
|
产品名称
|
包装
|
|
SC6542-10mM
|
K-115 (ROCK抑制剂)
|
10mM×0.2ml
|
|
SC6542-5mg
|
K-115 (ROCK抑制剂)
|
5mg
|
|
SC6542-25mg
|
K-115 (ROCK抑制剂)
|
25mg
|
|
—
|
说明书
|
1份
|
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
注意事项：
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。