PeptideDB

Netarsudil (AR-13324) 1254032-66-0

Netarsudil (AR-13324) 1254032-66-0

CAS No.: 1254032-66-0

Netarsudil (formerly known as AR-13324; AR13324; trade name Rhopressa) is ROCK inhibitor approved in 2017 for the treatm
Data collection：peptidedb@qq.com
Contact PeptideDB

This product is for research use only, not for human use. We do not sell to patients.

Netarsudil (formerly known as AR-13324; AR13324; trade name Rhopressa) is ROCK inhibitor approved in 2017 for the treatment of glaucoma and ocular hypertension. It inhibits ROCK with Ki of 0.2-10.3 nM. Netarsudil also inhibits norepinephrine transport activity which can reduce the production of aqueous humor. As of 2018, Netarsudil has been approved by FDA for the treatment of glaucoma and ocular hypertension. Previous study showed that at the cellular level, netarsudil was 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. Netarsudil primarily targets cells in the conventional outflow tract, efficiently decreasing IOP in both human and non-human primate eyes. In addition, netarsudil has been shown to increase outflow facility in non-human primate eyes and to decrease episcleral venous pressure in rabbit eyes.



Physicochemical Properties


Molecular Formula C28H27N3O3
Molecular Weight 453.54
Exact Mass 453.205
Elemental Analysis C, 74.15; H, 6.00; N, 9.27; O, 10.58
CAS # 1254032-66-0
Related CAS # 1422144-42-0 (mesylate);1254032-66-0;1253952-02-1 (HCl);
PubChem CID 66599893
Appearance White to off-white solid powder
Density 1.3±0.1 g/cm3
Boiling Point 711.9±60.0 °C at 760 mmHg
Flash Point 384.3±32.9 °C
Vapour Pressure 0.0±2.3 mmHg at 25°C
Index of Refraction 1.667
LogP 3.53
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 5
Rotatable Bond Count 8
Heavy Atom Count 34
Complexity 678
Defined Atom Stereocenter Count 1
SMILES

O(C(C1C=CC(C)=CC=1C)=O)CC1C=CC(=CC=1)[C@H](C(NC1C=CC2C=NC=CC=2C=1)=O)CN

InChi Key OURRXQUGYQRVML-AREMUKBSSA-N
InChi Code

InChI=1S/C28H27N3O3/c1-18-3-10-25(19(2)13-18)28(33)34-17-20-4-6-21(7-5-20)26(15-29)27(32)31-24-9-8-23-16-30-12-11-22(23)14-24/h3-14,16,26H,15,17,29H2,1-2H3,(H,31,32)/t26-/m1/s1
Chemical Name

Benzoic acid, 2,4-dimethyl-, (4-((1S)-1-(aminomethyl)-2-(6-isoquinolinylamino)-2-oxoethyl)phenyl)methyl ester
Synonyms

AR-13324; AR13324; Rhopressa; AR 13324; Netarsudil; 1254032-66-0; AR-11324 free base; Rhokiinsa; Rhopressa; Netarsudil [USAN]; UNII-W6I5QDT7QI; W6I5QDT7QI;
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month
Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity



Solubility Data



Dexanabinol 112924-45-5

Decoyinine 2004-04-8

Product Recommendation

Latest release

Hot list

Copyright © 2026 PeptideDB All Rights Reserved

Sitemaps | Contact

Is for research use only, not for human use. We do not sell to patients.

Targets Rho-associated protein kinas/ROCK; norepinephrine transporter/NET
Rho kinase; norepinephrine transporter [1]
Rho kinase; norepinephrine transporter [2]
ln 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.

Ex vivo perfusion of enucleated mouse eyes with netarsudil mesylate (100 nM) increased outflow facility compared to vehicle (0.001% DMSO) treatment. For C57BL/6 mice (n=8), the treatment led to a significant average increase in outflow facility (P=0.006), and for CD1 mice (n=6), a significant increase was also observed (P=0.025). The flow-pressure relationship was analyzed through 9 sequential pressure steps after 45-60 min of perfusion with the drug or vehicle [1]
Perfusion of enucleated human eyes with 0.3 μM netarsudil-M1 (active metabolite) at constant pressure (15 mmHg) for 3 hours significantly increased outflow facility (C) by 51% compared to baseline (P<0.01) and by 102% compared to paired vehicle controls (P<0.01). It also significantly increased the percentage effective filtration length (PEFL) in the inner wall (IW) of Schlemm's canal (SC) (P<0.05) and episcleral veins (ESVs) (P<0.01). In treated eyes, PEFL in ESVs was significantly higher than in IW (P<0.01) and positively correlated with the percentage change in C (R²=0.58, P=0.01). Additionally, the cross-sectional area of ESVs (P<0.01) and juxtacanalicular connective tissue (JCT) thickness (P<0.05) were significantly increased compared to controls [2]
ln Vivo Animal efficacy study found that the topical treatment of netarsudil was able to affect both proximal (trabecular meshwork and Schlemms Canal) and distal portions (intrascleral vessels) of the mouse conventional outflow tract.
Topical administration of 10 μl of 0.04% netarsudil mesylate to right eyes of 10-week-old C57 mice and 6-14 week-old CD1 mice (5 mice/group) significantly lowered intraocular pressure (IOP) compared to placebo (CF324-01) treatment (P<0.05 or P<0.01 for different strains) [1]
Intracameral preloading of 100 nM netarsudil mesylate into contralateral eyes of living mice (n=8) enhanced IOP recovery after artificial elevation to 40 mmHg. The rate constant α (characterizing pressure decay) was significantly increased compared to vehicle (0.001% DMSO) treatment (P<0.01) [1]
Topical netarsudil treatment in living C57 mice led to widening of the trabecular meshwork (TM) and a significant increase in the cross-sectional area of SC, as visualized by optical coherence tomography (OCT) imaging 45 min post-treatment. It also increased speckle variance intensity of outflow vessels, enhanced tracer deposition in conventional outflow tissues, and decreased IOP [1]
In living mice with elevated IOP, topical netarsudil treatment (10 μl of 0.04%) increased the cross-sectional area of SC lumen when IOP was controlled at 10, 15, and 30 mmHg (P<0.05 or P<0.01). OCT imaging showed significant changes in SC area relative to baseline (10 mmHg pre-treatment) in both C57 and CD1 mice (n=11) [1]
Topical netarsudil treatment in C57 and CD1 mice increased the cross-sectional area and speckle variance intensity of scleral vessels involved in aqueous humor outflow, as analyzed by OCT speckle variance images 30-60 min post-treatment (P<0.05) [1]
Enzyme Assay A total of 23 ROCK structures were found in the PDB. The maximum and minimum resolutions were 3.4 Å and 2.93 Å, respectively. Seven ROCK-I and two ROCK-II non-redundant structures were selected for the binding assay. Out of 46 compounds tested (20 isoquinolines, 15 aminofurazan, 6 benzodiazepine, 4 indazoles, and 1 amide), 34 presented a significantly higher docking score for ROCK-1, when compared to Y-27632 (p < 0.0001). All ROCKi classes presented a stronger mean docking score than Y-27632 (p < 0.0001). The frequency of compounds presenting highest docking score was higher in the isoquinoline, aminofurazan, and benzodiazepine classes for ROCK-I; and in isoquinolines and amides for ROCK-II (Supplementary Figure S2A). The top ten compounds that presented the highest mean docking scores for ROCK-I and II are shown in Supplementary Figure S2B. The isoquinoline class represented 70% of the drugs within the top ten highest docking scores, with three compounds presenting a docking score stronger than
Solubility (In Vitro)
DMSO: >10mM
Water:N/A
Ethanol:N/A
Solubility (In Vivo) Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
(e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders
Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2049 mL 11.0244 mL 22.0488 mL
5 mM 0.4410 mL 2.2049 mL 4.4098 mL
10 mM 0.2205 mL 1.1024 mL 2.2049 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.