Netarsudil
Based on 1 publication(s) in Google Scholar
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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.94%
- CAS 番号: 1254032-66-0
- 分子式: C28H27N3O3
- 分子量:453.53
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Netarsudil
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生物活性
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.
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Cell Line:Human trabecular meshwork cells
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Concentration:0.3 μM Netarsudil-M1
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Incubation Time:24 h
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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.
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.
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Animal Model:Male Dutch Belted rabbits (2.15±0.09 kg, male) episcleral venous pressure (EVP) and IOP measurement model[3]
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Dosage:0.04% Netarsudil ophthalmic solution (aqueous solution with 0.015% benzalkonium chloride)
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Administration:Topical instillation of 1 drop once daily for 3 days.
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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.
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Animal Model:Female cynomolgus monkeys (3-5 kg, female, adult) aqueous humor dynamics model[2]
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Dosage:0.04% Netarsudil ophthalmic solution (aqueous formulation).
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Administration:Topical instillation of 50 μL (25 μL×2) as a single dose
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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.
化学情報
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CAS 番号 1254032-66-0
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性状 Solid
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分子量 453.53
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分子式 C28H27N3O3
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Color White to off-white
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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
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別名
AR-13324
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Microbiol Spectr
Repurposing flufenamic acid as a putative PmrB-directed adjuvant to restore colistin activity in Klebsiella pneumoniae. [Abstract]2026 Mar 17:e0362025. PMID: 41842337
溶剤 & 溶解度
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.
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
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データシート (276 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
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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