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  3. Verosudil hydrochloride

Verosudil hydrochloride  (Synonyms: AR-12286 hydrochloride)

目录号: HY-16758A
产品使用指南 技术支持

Verosudil (AR-12286) hydrochloride 是 Verosudil (HY-16758) 的盐酸盐形式。Verosudil hydrochloride 是一种 ROCK 抑制剂。Verosudil hydrochloride 对 ROCK1ROCK2 具有相同的抑制活性 (Ki: 2 nM)。Verosudil hydrochloride 对 PKA、PKCT、MRCKA 和 CAM2A 的选择性较低 (Ki 分别为:69 nM、9322 nM、28 nM、5855 nM)。Verosudil hydrochloride 增加小梁流出能力来降低眼压。Verosudil hydrochloride 可用于青光眼和高眼压症的研究。

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Verosudil hydrochloride

Verosudil hydrochloride Chemical Structure

CAS No. : 1414854-44-6

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Verosudil hydrochloride 的其他形式现货产品:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Verosudil (AR-12286) hydrochloride is the hydrochloride form of Verosudil (HY-16758). Verosudil hydrochloride is a ROCK inhibitor. Verosudil hydrochloride has equal inhibitory activity against ROCK1 and ROCK2 (Ki: 2 nM). Verosudil hydrochloride is less selective for PKA, PKCT, MRCKA, and CAM2A (Ki: 69 nM, 9322 nM, 28 nM, 5855 nM, respectively). Verosudil hydrochloride increases trabecular outflow capacity to reduce intraocular pressure. Verosudil hydrochloride is useful in the study of glaucoma and ocular hypertension[1][2].

IC50 & Target

ROCK1

2 nM (Ki)

ROCK2

2 nM (Ki)

体外研究
(In Vitro)

Verosudil (AR-12286) hydrochloride 对 ROCK1ROCK2 具有相同的显著抑制活性 (Ki: 2 nM)[1]
Verosudil (0.001-100 μM,6 小时) hydrochloride 在猪原代小梁网细胞 (PTM) 中,剂量依赖性地减少肌动蛋白应力纤维的长度[1]
Verosudil (0.001-100 μM,6 小时) hydrochloride 在永生化的人小梁网细胞 (HTM) 中,减少黏着斑的数量[1]
Verosudil hydrochloride 在 PTM 细胞和 HTM 细胞中,具有破坏肌动蛋白应力纤维和粘着斑的能力 (分别为 IC50: 924 nM 和 IC50: 818 nM)[1]

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

体内研究
(In Vivo)

Verosudil (AR-12286) (30 μL,滴眼,每日一次,连续 3 天) hydrochloride 在荷兰带兔和台湾岩猴中,显著降低眼压[1]
Verosudil (10 μL,滴眼,每日两次,持续五周) hydrochloride 可以逆转 Dexamethasone (HY-14648) 诱发的眼高压小鼠模型的眼压、小梁网有效滤过面积和形态的变化[2]

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

Animal Model: Dexamethasone-induced ocular hypertension model in C57BL/6 mice (aged 6 weeks) [2]
Dosage: 10 μL
Administration: eye drops, twice daily for five weeks
Result: Reduced intraocular pressure in steroid-induce ocular hypertensive (SIOH) mice.
Increased the effective filtration area (EFA) in SIOH mouse eyes.
Reduced extracellular matrix (ECM) in eyes of SIOH mice.
Expanded the dense juxtatubular connective tissue (JCT) in the eyes of SIOH mice.
Clinical Trial
分子量

363.86

Formula

C17H18ClN3O2S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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Verosudil hydrochloride
目录号:
HY-16758A
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