K-115
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Ripasudil (K-115) 是一种新型的Rho激酶抑制剂，具有强效的降低眼压的效果。Rho激酶可被小GTP结合蛋白Rho激活。越来越多的证据表明，Rho/Rho激酶通路参与各种细胞功能，例如血管平滑肌细胞（VSMC）的收缩、肌动蛋白细胞骨架形成、细胞粘附和运动性、细胞分裂以及基因表达。这些功能障碍可能涉及诸如冠状动脉痉挛等心血管疾病的发病机理[1]。
在体实验：在视神经损伤（NC）的C57BL/6小鼠模型中，在NC后，口服K-115 (1 mg/kg/d) 增加了RGCs 34 ± 3％的存活率[2]。
临床试验：在I期临床试验中，滴注后2小时内进行测试，健康男性成年志愿者中，0.05％、0.1％、0.2％、0.4％和0.8％浓度的K-115使眼内压（IOP）从-1.6 mm汞柱下降至-3.4、-2.2、-2.6、-4.0和-4.3mm汞柱[3]。在2期原发性开角型青光眼或高眼压症的随机临床研究中，每日两次K-115，持续8周，K-115剂量依赖性地降低了眼压水平[4]。
参考文献：
Shimokawa H, Takeshita A. Rho-kinase is an important therapeutic target in cardiovascular medicine[J]. Arteriosclerosis, thrombosis, and vascular biology, 2005, 25(9): 1767-1775.
Yamamoto K, Maruyama K, Himori N, et al. The Novel Rho Kinase (ROCK) Inhibitor K-115: A New Candidate Drug for Neuroprotective Treatment in GlaucomaNovel Rho Kinase Inhibitor[J]. Investigative ophthalmology & visual science, 2014, 55(11): 7126-7136.
Tanihara H, Inoue T, Yamamoto T, et al. Phase 1 clinical trials of a selective Rho kinase inhibitor, K-115[J]. JAMA ophthalmology, 2013, 131(10): 1288-1295.
Tanihara H, Inoue T, Yamamoto T, et al. Phase 2 randomized clinical study of a Rho kinase inhibitor, K-115, in primary open-angle glaucoma and ocular hypertension[J]. American journal of ophthalmology, 2013, 156(4): 731-736. e2.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 395.88 |
| Cas No. | 887375-67-9 |
| Formula | C15H23ClFN3O4S |
| Solubility | insoluble in EtOH; ≥123.2 mg/mL in DMSO; ≥41.7 mg/mL in H2O |
| Chemical Name | 4-fluoro-5-[[(2S)-2-methyl-1,4-diazepan-1-yl]sulfonyl]isoquinoline;dihydrate;hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | CC1CNCCCN1S(=O)(=O)C2=CC=CC3=CN=CC(=C32)F.O.O.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
- 批次:
化学结构
