化学信息：
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化学名
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4-fluoro-5-[[(2S)-2-methyl-1,4-diazepan-1-yl]sulfonyl]isoquinoline
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简称
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K-115
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别名
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K115 compound, Glanatec, Ripasudil
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中文名
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N/A
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化学式
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C15H18FN3O2S
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分子量
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323.39
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CAS号
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223645-67-8
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纯度
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98%
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溶剂/溶解度
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Water<1mg/ml; DMSO4mg/ml; Ethanol<1mg/ml
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溶液配制
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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。
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生物信息：
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产品描述
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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.
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信号通路
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Cell Cycle; DNA Damage
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靶点
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ROCK
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－
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－
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－
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－
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IC50
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31nM
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－
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－
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－
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－
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体外研究
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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.
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体内研究
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N/A
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临床实验
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N/A
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特征
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N/A
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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)：
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酶活性检测实验
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方法
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N/A
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细胞实验
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细胞系
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N/A
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浓度
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N/A
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处理时间
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N/A
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方法
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N/A
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动物实验
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动物模型
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N/A
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配制
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N/A
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剂量
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N/A
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给药方式
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N/A
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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：
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产品编号
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产品名称
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包装
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SC6542-10mM
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K-115 (ROCK抑制剂)
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10mM×0.2ml
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SC6542-5mg
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K-115 (ROCK抑制剂)
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5mg
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SC6542-25mg
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K-115 (ROCK抑制剂)
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25mg
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—
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说明书
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1份
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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。
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