2. Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt Cytoskeleton
  3. ROCK
  4. Netarsudil hydrochloride

Netarsudil hydrochloride  (Synonyms: AR-13324 hydrochloride)

Cat. No.: HY-12798B Purity: 99.77%
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Handling Instructions Technical Support

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

For research use only. We do not sell to patients.

Netarsudil hydrochloride Chemical Structure

Netarsudil hydrochloride Chemical Structure

CAS No. : 1253952-02-1

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Based on 1 publication(s) in Google Scholar

Other Forms of Netarsudil hydrochloride:

Netarsudil hydrochloride Related Antibodies

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Description

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

IC50 & Target

ROCK, NET[1][2]
In Vitro

Netarsudil hydrochloride 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 hydrochloride Related Antibodies

Immunofluorescence[1]

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

Netarsudil hydrochloride (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 hydrochloride (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

526.45

Formula

C28H29Cl2N3O3
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.[H]Cl.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : ≥ 100 mg/mL (189.95 mM)

DMSO : 5 mg/mL (9.50 mM; Need ultrasonic; 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 1.8995 mL 9.4976 mL 18.9952 mL
5 mM 0.3799 mL 1.8995 mL 3.7990 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.77%

SDS (252 KB)

COA (246 KB) HNMR (274 KB) RP-HPLC (201 KB) MS (69 KB)

Handling Instructions (2659 KB)
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 (sealed storage, away from moisture). 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 / H2O 1 mM 1.8995 mL 9.4976 mL 18.9952 mL 47.4879 mL
5 mM 0.3799 mL 1.8995 mL 3.7990 mL 9.4976 mL
H2O 10 mM 0.1900 mL 0.9498 mL 1.8995 mL 4.7488 mL
15 mM 0.1266 mL 0.6332 mL 1.2663 mL 3.1659 mL
20 mM 0.0950 mL 0.4749 mL 0.9498 mL 2.3744 mL
25 mM 0.0760 mL 0.3799 mL 0.7598 mL 1.8995 mL
30 mM 0.0633 mL 0.3166 mL 0.6332 mL 1.5829 mL
40 mM 0.0475 mL 0.2374 mL 0.4749 mL 1.1872 mL
50 mM 0.0380 mL 0.1900 mL 0.3799 mL 0.9498 mL
60 mM 0.0317 mL 0.1583 mL 0.3166 mL 0.7915 mL
80 mM 0.0237 mL 0.1187 mL 0.2374 mL 0.5936 mL
100 mM 0.0190 mL 0.0950 mL 0.1900 mL 0.4749 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Netarsudil hydrochloride Related Classifications

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  • 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:

Netarsudil1253952-02-1AR-13324AR13324AR 13324ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKRho-associatedproteinkinasnorepinephrinetransporterNETintraocularpressureglaucomaInhibitorinhibitorinhibit

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