Netarsudil Dihydrochloride

SKU: orb1309987

Description

Netarsudil Dihydrochloride is a dual-action small molecule inhibitor targeting Rho kinase (ROCK) and the norepinephrine transporter (NET). It is widely used in ophthalmic research, particularly in studies investigating intraocular pressure (IOP) reduction, with applications in both in vitro and in vivo models of glaucoma.

Research Area

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1253952-02-1
• MW: 526.45
• Purity: 99.98% (May vary between batches)
• Formula: C₂₈H₂₉Cl₂N₃O₃
• SMILES: CC1=CC(=C(C=C1)C(=O)OCC2=CC=C(C=C2)[C@@H](CN)C(=O)NC3=CC4=C(C=C3)C=NC=C4)C.Cl.Cl
• Target: ROCK
• Solubility: DMSO:260 mg/mL (493.87 mM)

Bioactivity

• In Vivo:
  METHODS: Netarsudil 0.04% was administered once to one eye per animal for 3 days, with the untreated eye serving as a control. After dosing each morning on days 1 and 3, before test article administration (time 0) and at 1, 2, 4, 8 and 24 hours (rabbit) or 4, 8 and 24 hours (monkey) Intraocular pressure in both eyes. RESULTS Netarsudil 0.04% achieved greater IOP reduction and longer duration of efficacy. The greatest difference was seen 8 hours after dosing on Day 3, when Netarsudil 0.04% reduced IOP by 8.1 ± 0.7 mmHg.
• In Vitro:
  METHODS: Primary PTM cells were incubated for 6 hours in the presence of 0, 0.015, 0.138 or 1.2 μM Netarsudil, then fixed and stained with Alexa Fluor-488 phalloidin and Hoechst 33342, Netarsudil dosage in actin stress fiber assay reaction. RESULTS Netarsudil's ability to disrupt actin stress fibers and focal adhesions in PTM cells and HTM cells. METHODS: Serum-starved primary HTM cells were incubated for 24 hours in the presence of either vehicle, fixed and stained for fibrosis markers with 8 ng/mL human TGF-β2, 500 nM netarsudil or 8 ng/mL TGF-β2 plus 500 nM netarsudil. α-SMA, fibroblast-specific protein 1 (FSP1) and collagen 1A were used to explore the effect of Netarsudil on the profibrotic effect of TGF-β on HTM cells. RESULTS Simultaneous treatment of HTM cells with TGF-β2 and Netarsudil abolished the induction of these markers by TGF-β2, indicating that Netarsudil has antifibrotic activity.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ROCK, Netarsudil, Netarsudil Dihydrochloride, AR13324 Dihydrochloride, AR-13324 Dihydrochloride, AR13324, AR-13324, AR 13324, AR 13324 Dihydrochloride

Compound Identifiers

PubChem CID

66599892