Hydroxyfasudil HCl

製品コードS8208 バッチS820802

印刷

化学情報

Synonyms

HA-1100

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₄H₁₇N₃O₃S·HCl·xH₂O

分子量

343.83

CAS No.

155558-32-0

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

11 mg/mL (31.99 mM)

Water (warmed with 50ºC water bath)

8 mg/mL (23.26 mM)

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.550mg/ml (1.60mM)	Taking the 1 mL working solution as an example, add 50 μL of 11 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.550mg/ml (1.60mM)	Taking the 1 mL working solution as an example, add 50 μL of 11 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Hydroxyfasudil HCl, an active metabolite of fasudil hydrochloride, is a specific Rho-kinase(ROCK) inhibitor with IC50 values of 0.73 μM and 0.72 μM for ROCK1 and ROCK2, respectively.
in vitro	Hydroxyfasudil prevents the downregulation of endothelial NO synthase (eNOS) under hypoxic conditions. In a concentration-dependent manner, hydroxyfasudil increases eNOS mRNA and protein expression, resulting in a 1.9- and 1.6-fold increase, respectively, at 10 μmol/L (P<0.05 for both). This correlates with a 1.5- and 2.3-fold increase in eNOS activity and NO production, respectively (P<0.05 for both)^[1]. Hydroxyfasudil also inhibits various chemoattractant-induced migration of neutrophils. Hydroxyfasudil potently inhibits Rho-kinase (IC50, 0.9 ± 1.8 μM), while its inhibitory effect is markedly (at least 50 ± 100 times) less for myosin light chain kinase (MLCK) or protein kinase C (PKC)^[3].
in vivo	Intracoronary administration of hydroxyfasudil(HF) causes a significant coronary vasodilation of both small arteries and arterioles in a dose-dependent manner under control conditions with a resultant increase in CBF(coronary blood flow). Intracoronary hydroxyfasudil does not significantly alter mean aortic pressure or heart rate. Pretreatment with hydroxyfasudil markedly reduces the I/R-induced myocardial infarct size, and this beneficial effect of hydroxyfasudil is significantly attenuated by L-NMMA. NO may be involved in those cardiovascular protective effects of hydroxyfasudil. Hydroxyfasudil may also be effective for the treatment of pulmonary hypertension^[2]. HF protects the myocardium subjected to pacing-induced ischaemia through the increase in the regional myocardial blood flow^[3].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Human vascular endothelial cells
	濃度	0.1 to 100 μmol/L
	反応時間	18 h
	実験の流れ	Human vascular endothelial cells are treated with increasing concentrations of hydroxyfasudil (0.1 to 100 μmol/L) and eNOS expression and activity are measured.
動物実験	動物モデル	Mongrel dogs
	投薬量	10, 30, and 100 μg/kg
	投与方法	IC（Intracoronary administration）

参考

https://pubmed.ncbi.nlm.nih.gov/16141422/
https://pubmed.ncbi.nlm.nih.gov/15708710/
http://pubmedcentralcanada.ca/pmcc/articles/PMC1572897/pdf/134-0704410a.pdf

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Drug and siRNA screens identify ROCK2 as a therapeutic target for ciliopathies [ Commun Med (Lond), 2025, 5(1):129]	PubMed: 40253509
Pixantrone as a novel MCM2 inhibitor for ovarian cancer treatment [ Eur J Pharmacol, 2024, 979:176835]	PubMed: 39032764
Drug and siRNA screens identify ROCK2 as a therapeutic target for ciliopathies [ bioRxiv, 2020, 10.1101/2020.11.26.393801]	PubMed: N/A

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。