Netarsudil (dimesylate)

Netarsudil (AR-13324) dimesylate is a competitive inhibitor of Rho-associated protein kinases (ROCK I and ROCK II) and a reversible inhibitor of the norepinephrine transporter (NET) . Netarsudil dimesylate reduces intraocular pressure by inhibiting ROCK, causing relaxation of trabecular meshwork cells and dilation of episcleral veins, thereby increasing the ease of aqueous humor outflow, while inhibiting NET to reduce aqueous humor production. Netarsudil dimesylate is mainly used in the study of ocular hypertension and primary open-angle glaucoma[1][2][3][4].

Product Specifications

CAS Number

[1422144-42-0]

Product Name Alternative

AR-13324 (dimesylate)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

ROCK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Cytoskeleton; Stem Cell/Wnt; TGF-beta/Smad

Field of Research

Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/Netarsudil_mesylate.html

Purity

99.90

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CC1=CC(C)=C(C(OCC2=CC=C([C@@H](CN)C(NC3=CC(C=CN=C4)=C4C=C3)=O)C=C2)=O)C=C1.CS(=O)(O)=O.CS(=O)(O)=O

Molecular Formula

C30H35N3O9S2

Molecular Weight

645.74

Precautions

H302, H315, H319, H335

References & Citations

[1]Ren R, et al. Netarsudil Increases Outflow Facility in Human Eyes Through Multiple Mechanisms. Invest Ophthalmol Vis Sci. 2016 Nov 1;57 (14) :6197-6209.|[2]Wang RF, et al. Effect of 0.04% AR-13324, a ROCK, and norepinephrine transporter inhibitor, on aqueous humor dynamics in normotensive monkey eyes. J Glaucoma. 2015 Jan;24 (1) :51-54.|[3]Kiel JW, et al. Effect of AR-13324 on episcleral venous pressure in Dutch belted rabbits. J Ocul Pharmacol Ther. 2015 Apr;31 (3) :146-151.|[4]Chen S, et al. Dose-dependent effects of netarsudil, a Rho-kinase inhibitor, on the distal outflow tract. Graefes Arch Clin Exp Ophthalmol. 2020 Jun;258 (6) :1211-1216.