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

Netarsudil hydrochloride  (Synonyms: AR-13324 hydrochloride)

目录号: HY-12798B 纯度: 99.90%
COA 产品使用指南 技术支持

Netarsudil (AR-13324) hydrochloride 是一种 Rho 相关蛋白激酶 (ROCK I 和 ROCK II) 的竞争性抑制剂，以及去甲肾上腺素转运体 (NET) 的可逆抑制剂。Netarsudil hydrochloride 通过抑制 ROCK 使小梁网细胞松弛、episcleral 静脉扩张，从而增加房水 (aqueous humor) 外流易度，同时抑制 NET 减少房水生成来降低眼压。Netarsudil hydrochloride 主要用于高眼压症和原发性开角型青光眼的研究。

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Netarsudil hydrochloride Chemical Structure

Netarsudil hydrochloride Chemical Structure

CAS No. : 1253952-02-1

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规格 价格 是否有货 数量
1 mg ￥985
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2 mg ￥1400
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5 mg ￥2800
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10 mg ￥4488
In-stock
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Customer Review

Other Forms of Netarsudil hydrochloride:

Netarsudil hydrochloride 相关抗体

Top Publications Citing Use of Products

查看 ROCK 亚型特异性产品:

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ROCK ROCK1 ROCK2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]
体外研究
(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].

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

Netarsudil hydrochloride 相关抗体:

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.
体内研究
(In Vivo)

Netarsudil hydrochloride (0.04%，50 毫升) 可降低正常眼压猴的眼压 (IOP)[1]。
Netarsudil hydrochloride (0.04%) 可显著降低荷兰带兔的巩膜上静脉压 (EVP)[2]。

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.
Clinical Trial
分子量

526.45

Formula

C28H29Cl2N3O3
CAS 号
性状

固体

颜色

White to off-white

中文名称

盐酸奈他地尔
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
细胞实验： 

H2O 中的溶解度 : ≥ 100 mg/mL (189.95 mM)

DMSO 中的溶解度 : 5 mg/mL (9.50 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.90%

COA (284 KB) HNMR (272 KB) LCMS (94 KB)

产品使用指南 (1538 KB)
参考文献

Netarsudil hydrochloride 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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:

Netarsudil1253952-02-1AR-13324盐酸奈他地尔AR13324AR 13324ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKRho-associatedproteinkinasnorepinephrinetransporterNETintraocularpressureglaucomaInhibitorinhibitorinhibit

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