Netarsudil hydrochloride
Based on 1 publication(s) in Google Scholar
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.
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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: 99.90%
- CAS 番号: 1253952-02-1
- 分子式: C28H29Cl2N3O3
- 分子量:526.45
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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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MedChemExpress（MCE）の使用を引用している文献 Netarsudil hydrochloride
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生物活性
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.
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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: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.
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.
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1253952-02-1
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性状 Solid
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分子量 526.45
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分子式 C28H29Cl2N3O3
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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.[H]Cl.[H]Cl
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別名
AR-13324 hydrochloride
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
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.
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
純度とドキュメンテーション
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データシート (278 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 (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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