中文名稱:K115 | 英文名稱:K115 |
CAS:887375-67-9 | 有效期: 一個月 |
K-115, an isoquinolinesulfonamide compound, is a highly selective and potent (IC50 = 31 nM) Rho-kinase inhibitor; is in Phase II clinical development in patients with POAG or ocular hypertension.
IC50 value: 31 nM [1]
Target: ROCK inhibitor
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 1?h after topical instillation, which was 8.55?±?1.09?mmHg (mean?±?SE) from the baseline IOP at 0.5%. In monkeys, maximum IOP reduction was observed 2?h after topical instillation, which was 4.36?±?0.32?mmHg 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 15?min after instillation of [(14)C]K-115 in the ipsilateral eye [3].
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 [4].
成立日期 | 2016-04-18 (9年) | 注冊資本 | 100萬人民幣 |
員工人數(shù) | 年營業(yè)額 | ||
主營行業(yè) | 化學(xué)試劑,醫(yī)藥中間體,分子砌塊,原料藥,天然化學(xué)藥 | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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