2. Membrane Transporter/Ion Channel Stem Cell/Wnt Cytoskeleton Cell Cycle/DNA Damage TGF-beta/Smad
  3. Monoamine Transporter ROCK
  4. Netarsudil

Netarsudil (AR-13324) is a competitive inhibitor of Rho-associated protein kinases (ROCK I and ROCK II) and a reversible inhibitor of the norepinephrine transporter (NET). Netarsudil 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 is mainly used in the study of ocular hypertension and primary open-angle glaucoma.

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Netarsudil Chemical Structure

Netarsudil Chemical Structure

CAS No. : 1254032-66-0

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Based on 1 publication(s) in Google Scholar

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Netarsudil Related Antibodies

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Description

Netarsudil (AR-13324) is a competitive inhibitor of Rho-associated protein kinases (ROCK I and ROCK II) and a reversible inhibitor of the norepinephrine transporter (NET). Netarsudil 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 is mainly used in the study of ocular hypertension and primary open-angle glaucoma[1][2][3][4].

In Vitro

Netarsudil exerts its effects by metabolizing to the active compound Netarsudil-M1. Netarsudil-M1 (0.3 μM; 3 h) significantly increases aqueous humor outflow ease in human ocular tissue perfusion experiments and increases effective filtration length (PEFL) by dilating the trabecular meshwork (TM) and episcleral veins (ESV)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Netarsudil Related Antibodies

Immunofluorescence[1]

Cell Line: Human trabecular meshwork cells
Concentration: 0.3 μM Netarsudil-M1
Incubation Time: 24 h
Result: Reduced formation of actin stress fibers and focal adhesions, accompanied by cell rounding and detachment, indicative of relaxed cell contractility.
Decreased phosphorylation of myosin light chain (MLC), a marker of ROCK-mediated contraction, confirming inhibition of the Rho-kinase pathway.
In Vivo

Netarsudil (0.04% ophthalmic solution; topical instillation; single dose) increases aqueous humor outflow ease and reduces aqueous humor production after 6 hours of treatment in female cynomolgus monkeys, exerting an ocular hypotensive effect[2].
Netarsudil (0.04% eye drops; topical instillation; once daily; 3 days) significantly reduces intraocular pressure and episcleral venous pressure in male Dutch DB rabbits without affecting arterial pressure, heart rate, and carotid blood flow[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Dutch Belted rabbits (2.15±0.09 kg, male) episcleral venous pressure (EVP) and IOP measurement model[3]
Dosage: 0.04% Netarsudil ophthalmic solution (aqueous solution with 0.015% benzalkonium chloride)
Administration: Topical instillation of 1 drop once daily for 3 days.
Result: Baseline values: IOP 34±4 mmHg, EVP 17±2 mmHg, arterial pressure (AP) 105±3 mmHg, carotid blood flow (BFcar) 35±1 mL/min, heart rate (HR) 337±9 bpm.
Three hours after the final dose, IOP decreased by 39% to 19±2 mmHg, EVP decreased by 35% to 11±1 mmHg.
AP, BFcar, and HR showed no significant changes throughout the experiment, indicating no systemic hemodynamic effects.
Animal Model: Female cynomolgus monkeys (3-5 kg, female, adult) aqueous humor dynamics model[2]
Dosage: 0.04% Netarsudil ophthalmic solution (aqueous formulation).
Administration: Topical instillation of 50 μL (25 μL×2) as a single dose
Result: Six hours post-treatment, outflow facility (C) increased by 53% compared to baseline, from 0.58±0.07 to 0.90±0.11 μL/min/mmHg.
Aqueous humor flow rate (F) decreased by 23% compared to baseline, from 1.60±0.11 to 1.25±0.19 μL/min.
IOP was reduced by 25% compared to baseline, with no significant changes observed in contralateral vehicle-treated eyes.
Molecular Weight

453.53

Formula

C28H27N3O3
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (220.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2049 mL 11.0246 mL 22.0493 mL
5 mM 0.4410 mL 2.2049 mL 4.4099 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2049 mL 11.0246 mL 22.0493 mL 55.1231 mL
5 mM 0.4410 mL 2.2049 mL 4.4099 mL 11.0246 mL
10 mM 0.2205 mL 1.1025 mL 2.2049 mL 5.5123 mL
15 mM 0.1470 mL 0.7350 mL 1.4700 mL 3.6749 mL
20 mM 0.1102 mL 0.5512 mL 1.1025 mL 2.7562 mL
25 mM 0.0882 mL 0.4410 mL 0.8820 mL 2.2049 mL
30 mM 0.0735 mL 0.3675 mL 0.7350 mL 1.8374 mL
40 mM 0.0551 mL 0.2756 mL 0.5512 mL 1.3781 mL
50 mM 0.0441 mL 0.2205 mL 0.4410 mL 1.1025 mL
60 mM 0.0367 mL 0.1837 mL 0.3675 mL 0.9187 mL
80 mM 0.0276 mL 0.1378 mL 0.2756 mL 0.6890 mL
100 mM 0.0220 mL 0.1102 mL 0.2205 mL 0.5512 mL
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Netarsudil Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Netarsudil1254032-66-0AR-13324AR13324AR 13324Monoamine TransporterROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKoutflow facilityeyesInhibitorinhibitorinhibit

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