Netarsudil (AR-13324)
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.
Ki为0.2-10.3 nM。
Netarsudil(AR-13324)是ROCK抑制剂。
Rho激酶是作为ROCK1和ROCK2两种同种型存在的丝氨酸/苏氨酸蛋白激酶,在多种组织(例如小梁网)中广泛表达。ROCK可以促进肌动蛋白应力纤维和黏着斑的组装,并且还可以调节细胞收缩和运动。
体外:先前的研究表明,netarsudil在细胞水平能够诱导肌动蛋白应力纤维损失、细胞形状变化、黏着斑损失,以及TM细胞的细胞外基质组成的变化[1] 。
体内:动物功效研究发现,netarsudil局部治疗能够影响小鼠常规流出道的近端(小梁网和Schlemm管)以及远端部分(巩膜内管)[2]。
临床试验:先前两项II期临床试验表明,在青光眼和高眼压患者服药四周后,0.02%的netarsudil治疗产生显著的范围为5.7-6.3 mmHg 的DIOP。此外,研究发现netarsudil耐受性良好,最常报道的不良事件为轻微充血。目前,netarsudil处于治疗高眼压和开角型青光眼的III期临床试验中[1]。
参考文献:
[1] Sturdivant JM et al. Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma. Bioorg Med Chem Lett.2016 May 15;26(10):2475-80.
[2] Li G et al. Visualization of conventional outflow tissue responses to netarsudil in living mouse eyes. Eur J Pharmacol.2016 Sep 15;787:20-31.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 526.45 |
Cas No. | 1253952-02-1 |
Formula | C28H29Cl2N3O3 |
Solubility | ≥26.3 mg/mL in H2O with gentle warming and ultrasonic; insoluble in EtOH; ≥7.783 mg/mL in DMSO |
Chemical Name | (R)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate dihydrochloride |
SDF | Download SDF |
Canonical SMILES | [H]Cl.[H]Cl.O=C(OCC1=CC=C([C@H](CN)C(NC2=CC3=C(C=NC=C3)C=C2)=O)C=C1)C4=CC=C(C)C=C4C |
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
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