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Hydroxyfasudil

Name: Hydroxyfasudil
Brand: TargetMol
SKU: T4276L
Price: 127 CNY
Availability: InStock
Rating: 5 (10 reviews)

一键复制产品信息

很棒

纯度: 98.13%

货号 T4276LCas号 105628-72-6

别名 羟基法舒地尔, Hydroxy-Fasudil, HA-1100

Hydroxyfasudil (Hydroxy-Fasudil) 是一种ROCK 抑制剂，对ROCK1和ROCK2的IC50分别为 0.73 和 0.72 μM。

Hydroxyfasudil

一键复制产品信息

很棒

纯度: 98.13%

货号 T4276L 别名 羟基法舒地尔, Hydroxy-Fasudil, HA-1100Cas号 105628-72-6

Hydroxyfasudil (Hydroxy-Fasudil) 是一种ROCK 抑制剂，对ROCK1和ROCK2的IC50分别为 0.73 和 0.72 μM。

规格	价格	库存
1 mg	¥ 127	现货
5 mg	¥ 322	现货
10 mg	¥ 498	现货
25 mg	¥ 972	现货
50 mg	¥ 1,550	现货
100 mg	¥ 2,290	现货
1 mL x 10 mM (in DMSO)	¥ 217	现货

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实验操作小课堂

常见问题解答

选择批次:

纯度: 98.13%

颜色: 白色

性状: Solid

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资源下载:

COA HNMR LCMS 产品操作手册

产品介绍

Hydroxyfasudil AI Summary

Hydroxyfasudil is a multifaceted inhibitor with significant bioactivity against various enzymes and possesses antiviral properties. It exhibits notable selectivity for ROCK1 over PKA, with a Ki of 150.0 nM against ROCK1 and 2200.0 nM against PKA, resulting in a selectivity ratio of 15.0. Additionally, it inhibits human ROCK1 and ROCK2 with IC50 values of 758.58 nM and 575.44 nM, respectively, and demonstrates inhibition of ROCK-1 with a Ki value of 31.62 nM. Beyond its activity on ROCK enzymes, Hydroxyfasudil also inhibits Cruzain (4466.8 nM), Aldehyde Dehydrogenase 1 (ALDH1A1) (23755.8 nM), and HPGD (15-Hydroxyprostaglandin Dehydrogenase) (14125.4 nM). It further shows activity against human ERG with a Ki of 7943.28 nM and reduces MCP1-mediated human THP cell migration with an IC50 of 6918.31 nM. The compound demonstrates oral bioavailability in C57 mice at 57.0%, a clearance rate of 34.0 mL.min-1.kg-1, volume of distribution at steady state of 2.4 L.kg-1, and a half-life of 0.75 hours. Additionally, it shows good kinetic solubility in pH 7.4 PBS buffer (> 200000.0 nM) and a logP value of 1.43. In terms of antiviral activity, Hydroxyfasudil inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 cells at a concentration of 10 µM with an inhibition rate of 7.36% and shows efficacy against the SARS-CoV-2 3CL-Pro protease at 20 µM with inhibition rates of 18.62% and 8.854%. It also has measurable inhibition against HDAC6, with percentages of 9.53% and 8.82% using different substrates. Lastly, it demonstrates inhibition of PARP1 with an IC50 value of 27,000.0 nM and has shown antiinvasive activity in human HT1080 cells at 50 µM with an activity of 50.0%..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Hydroxyfasudil (Hydroxy-Fasudil) is a ROCK inhibitor(IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively).
靶点活性	ROCK2:0.72 μM, ROCK1:0.73 μM, PKA:37 μM
别名	羟基法舒地尔, Hydroxy-Fasudil, HA-1100

化学信息

分子量	307.37
分子式	C₁₄H₁₇N₃O₃S
CAS No.	105628-72-6
Smiles	O=c1[nH]ccc2c(cccc12)S(=O)(=O)N1CCCNCC1
密度	1.329g/cm3

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 31 mg/mL (100.86 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 0.5 mg/mL (1.63 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.2534 mL	16.2670 mL	32.5341 mL	162.6704 mL
5 mM	0.6507 mL	3.2534 mL	6.5068 mL	32.5341 mL
10 mM	0.3253 mL	1.6267 mL	3.2534 mL	16.2670 mL
20 mM	0.1627 mL	0.8134 mL	1.6267 mL	8.1335 mL
50 mM	0.0651 mL	0.3253 mL	0.6507 mL	3.2534 mL
100 mM	0.0325 mL	0.1627 mL	0.3253 mL	1.6267 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：

比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH₂O，那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 100 μL DMSO （母液浓度为 20 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法： 取 100 μL DMSO 母液，添加 400 μL PEG300 混匀澄清，再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH₂O 混匀澄清

以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。

方案所需的各类助溶剂如： DMSO， PEG300， PEG400， Tween 80， SBE-β-CD，玉米油等，均可在TargetMol网站点击购买。

剂量转换

对于不同动物的给药剂量换算，您也可以参考更多

关键词

ROK ROCK2 ROCK1 ROCK Rho-kinase Rho-associated protein kinase Rho-associated kinase PKA Inhibitor inhibit Hydroxyfasudil HA1100 HA 1100

Hydroxyfasudil

Hydroxyfasudil

Hydroxyfasudil 相关产品

产品介绍

计算器

体内实验配液计算器

剂量转换

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