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Netarsudil 2HCl(AR-13324)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Netarsudil 2HCl(AR-13324)图片
CAS NO:1253952-02-1
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)526.45
FormulaC28H27N3O3.2HCl
CAS No.1253952-02-1 (DiHCl);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 20 mg/mL (38 mM)
Water: 54 mg/mL (102.6 mM)
Ethanol: 2 mg/mL (3.8 mM)
SMILES CodeO=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.[H]Cl.[H]Cl
Synonyms

AR13324 HCl; Rhopressa; AR-13324 HCl; AR 13324; AR 13324 HCl; Netarsudil; AR-13324; Netarsudil hydrochloride

Chemical Name: [4-[(2S)-3-Amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl]phenyl]methyl 2,4-dimethylbenzoate dihydrochloride

Exact Mass: 525.1586

实验参考方法
In Vitro

In vitro activity: Previous study showed that at the cellular level, netarsudil had been shown to be able to induce loss of actin stress fibers, cell shape changes, loss of focal adhesions, as well as changes in extracellular matrix composition of TM cells


Kinase Assay: Netarsudil (formerly known as AR-13324) is ROCK inhibitor with Ki of 0.2-10.3 nM. It also inhibits norepinephrine transport activity which can reduce the production of aqueous humor.


Cell Assay: Previous study showed that at the cellular level, netarsudil had been shown to be able to induce loss of actin stress fibers, cell shape changes, loss of focal adhesions, as well as changes in extracellular matrix composition of TM cells.

In VivoAnimal efficacy study found that the topical treatment of netarsudil was able to affect both proximal (trabecular meshwork and Schlemm's Canal) and distal portions (intrascleral vessels) of the mouse conventional outflow tract.
Animal modelMice with elevated intraocular pressure (IOP)
Formulation & DosageTopical application
ReferencesEur J Pharmacol. 2016 Sep 15;787:20-31; Invest Ophthalmol Vis Sci. 2016 Nov 1;57(14):6197-6209.