1253952-02-1

Basic information

• Product Name: AR-13324 (hydrochloride)
• Synonyms: AR-13324 (hydrochloride);Netarsudil hydrochloride;2,4-Dimethylbenzoic acid [4-[(1S)-1-(aminomethyl)-2-(6-isoquinolinylamino)-2-oxoethyl]phenyl]methyl ester hydrochloride (1:2);Netarsudil;AR-13324 hydrochloride:AR13324 hydrochloride;AR-13324
• CAS NO: 1253952-02-1
• Molecular Formula: C28H29Cl2N3O3
• Molecular Weight: 526.45416
• Mol File: 1253952-02-1.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• Solubility: ≥26.3 mg/mL in H2O with gentle warming and ultrasonic; insoluble in EtOH; ≥7.783 mg/mL in DMSO
• CAS DataBase Reference: AR-13324 (hydrochloride)(CAS DataBase Reference)
• NIST Chemistry Reference: AR-13324 (hydrochloride)(1253952-02-1)
• EPA Substance Registry System: AR-13324 (hydrochloride)(1253952-02-1)

Safety Data

• Hazardous Substances Data: 1253952-02-1(Hazardous Substances Data)

Usage

Biological Activity

ki: 0.2-10.3 nmnetarsudil (ar-13324) is a rock inhibitor.the rho kinases are serine/threonine protein kinases existing as 2 isoforms, rock1 and rock2, which are widely expressed in various tissues, such as the trabecular meshwork. rock can promote the assembly of actin stress fibers and focal adhesions and can also regulate cell contraction and motility.

in vitro

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 [1].

in vivo

animal 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 [2].

references

[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.