Netarsudil (AR-13324)
(Synonyms: 2,4-二甲基苯甲酸[4-[(1S)-1-(氨基甲基)-2-(6-异喹啉基氨基)-2-氧代乙基]苯基]甲基酯二盐酸盐) 目录号 : GC10716
ROCK抑制剂
Cas No.:1253952-02-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ki: 0.2-10.3 nM
Netarsudil (AR-13324) is a ROCK inhibitor.
The Rho kinases are serine/threonine protein kinases existing as 2 isoforms, ROCK1 and ROCK2, which are widely expressed in various tissues, such as the trabecular meshwork. ROCK can promote the assembly of actin stress fibers and focal adhesions and can also regulate cell contraction and motility.
In vitro: Previous study showed that at the cellular level, netarsudil had been shown to be able to induce loss of actin stress fibers, cell shape changes, loss of focal adhesions, as well as changes in extracellular matrix composition of TM cells [1].
In vivo: Animal efficacy study found that the topical treatment of netarsudil was able to affect both proximal (trabecular meshwork and Schlemm's Canal) and distal portions (intrascleral vessels) of the mouse conventional outflow tract [2].
Clinical trial: Previous two phase II clinical trials showed that netarsudil 0.02% treatment was shown to produce significant DIOPs that ranged from 5.7 to 6.3 mmHg after four weeks of dosing in patients with glaucoma and ocular hypertension. In addition, it was found that netarsudil was well tolerated, with trace to mild hyperemia being the most frequently reported adverse event. Currently, netarsudil is in phase III clinical trials for the treatment of ocular hypertension and open-angle glaucoma [1].
References:
[1] Sturdivant JM et al. Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma. Bioorg Med Chem Lett. 2016 May 15;26(10):2475-80.
[2] Li G et al. Visualization of conventional outflow tissue responses to netarsudil in living mouse eyes. Eur J Pharmacol. 2016 Sep 15;787:20-31.
| Cas No. | 1253952-02-1 | SDF | |
| 别名 | 2,4-二甲基苯甲酸[4-[(1S)-1-(氨基甲基)-2-(6-异喹啉基氨基)-2-氧代乙基]苯基]甲基酯二盐酸盐 | ||
| 化学名 | (R)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate dihydrochloride | ||
| Canonical SMILES | [H]Cl.[H]Cl.O=C(OCC1=CC=C([C@H](CN)C(NC2=CC3=C(C=NC=C3)C=C2)=O)C=C1)C4=CC=C(C)C=C4C | ||
| 分子式 | C28H29Cl2N3O3 | 分子量 | 526.45 |
| 溶解度 | ≥ 26.3mg/mL in Water with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 | 3.799 mL |
| 10 mM | 0.19 mL | 0.9498 mL | 1.8995 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。