ホームページ Cell Cycle ROCK inhibitor - Autophagy activator - PKA inhibitor - PKC inhibitor - MLCK inhibitor - Rho inhibitor - Calcium Channel inhibitor - PKG inhibitor Fasudil HCl For research use only.

Fasudil HCl

別名：AT-877,HA-1077 HCl

Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.

Fasudil HCl化学構造

CAS No. 105628-07-7

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 37000 国内在庫なし(納期7~10日)
JPY 59500 国内在庫あり

代表番号: 045-509-1970|電子メール：[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例（82）

製品安全説明書

現在のバッチを見る： 純度： 99.99%
99.99

Fasudil HClと併用されることが多い化合物

Ozagrel sodium

Fasudil HCl and Ozagrel sodium have superior effectiveness over only ozagrel sodium in treating patients at risk of vasospasm after aneurysmal subarachnoid hemorrhage.

Nakashima S, et al. Neurol Med Chir (Tokyo). 1998 Dec;38(12):805-10; discussion 810-1.

Methylcobalamin

Fasudil and Methylcobalamin combination therapy improves neuropathic symptoms and nerve conduction velocity in patients with diabetic peripheral neuropathy (DPN).

Jiang DQ, et al. Medicine (Baltimore). 2018 Jul; 97(27): e11390.

Fasudil HCl関連製品

シグナル伝達経路

ROCK Signaling Pathways

ROCKシグナル伝達経路

ROCK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
insect cells Function assay 10 mins Inhibition of human leukocytic ROCK1 expressed in insect cells using KKRNRTLSV as substrate after 10 mins by pyruvate kinase/lactate dehydrogenase coupled assay, Ki=0.53 μM. 26039570
Sf9 cells Function assay 90 mins Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 substrate and [gamma-33P]ATP after 90 mins by scintillation proximity assay, IC50=0.3 μM. 17018693
Sf9 cells Function assay Inhibition of rat ROCK2 expressed in Sf9 cells, IC50=1.9 μM. 10998351
HEK293 cells Function assay Inhibition of His-tagged human PRK2 expressed in HEK293 cells, IC50=4 μM. 10998351
U937 cells Function assay Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2, IC50=35 μM. 17084087
Sf9 cells Function assay Inhibition of His-tagged human MSK1 expressed in Sf9 cells, IC50=5 μM. 10998351
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明 Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.
Targets
Rho [1] Calcium channel [2] ROCK2 [1]
(Cell-free assay)		 PKA [1]
(Cell-free assay)		 PKG [1]
(Cell-free assay)		 もっとクリックする
330 nM(Ki) 1.6 μM(Ki) 1.6 μM(Ki)
In Vitro
In vitro

Fasudil is a class of calcium antagonists. Fasudil produces a competitive inhibition of the Ca2+-induced contraction of the depolarized rabbit aorta. Fasudil is able to inhibit contractile responses to KCl, phenylephnne (PHE) and prostaglandin (PG) F2a. [2]

Fasudil also exhibits vasodilator actions by inhibition of 5-hydroxytryptamine, noradrenaline, histamine, angiotensin, and dopamine induced spiral strips contraction. [3]

Fasudil induces disorganization of actin stress fiber and cell migration inhibition. [4]

Fasudil inhibits hepatic stellate cells spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth, but does not induce apoptosis. Fasudil suppresses the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK. [5]
Kinase Assay Cyclic AMP-dependent protein kinase activity assay
Cyclic AMP-dependent protein kinase activity is assayed in a reaction mixture containing, in a final volume of 0.2 mL, 50 mM Tris-HCl (pH 7.0), 10 mM magnesium acetate, 2 mM EGTA, 1 μM cyclic AMP or absence of cyclic AMP, 3.3 to 20 μM [r-32P] ATP (4×105 c.p.m.), 0.5 μg of the enzyme, 100 μg of histone H2B and compound. The mixture is incubated at 30 ℃ for 5 min. The reaction is terminated by adding 1mL of ice-cold 20% trichloroacetic acid after adding 500 μg of bovine serum albumin as a carrier protein. The sample is centrifuged at 3000 r.p.m. for 15min, the pellet is resuspended in ice-cold 10% trichloro-acetic acid solution and the centrifugation-resuspension cycle is repeated three times. The final pellet is dissolved in 1 mL of 1 N NaOH and radioactivity is measured with a liquid scintillation counter.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot ROCK2 / p-ROCK2 / MLC2 / p-MLC2 ABCG2 Moesin / p-Moesin / β-catenin / p-β-catenin 29416017
Immunofluorescence p-ROCK2 / ABCG2 29416017
Growth inhibition assay Cell viability 29262624
In Vivo
In Vivo

Intra-coronary injection of Fasudil to dogs (30 μg i.a.) produces an approximate 50% increase in CBF. Fasudil (0.01, 0.03, 0.1 and 0.3 mg/kg, bolus, i.v.) dose-dependently decreases MBP and increases HR, VBF, CBF, RBF, and FBF. A total dose of 1.0 ng/mL Fasudil increases cardiac output. The infusion of Fasudil i.v. produces a significant fall in MBP, left ventricular systolic pressure and total peripheral resistance with an increase in HR and cardiac output, but without significant changes in right atrial pressure, dP/dt or left ventricular minute work in dogs. [3]

Fasudil administration displays protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury. [6]

The oral administration of Fasudil (a dosage of 100 mg/kg/day) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Treatment of mice with Fasudil suppresses the proliferative response of splenocytes to the antigen. Oral administration of Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice. [7]
動物実験 動物モデル Mongrel dogs
投与量 0.01, 0.03, 0.1 and 0.3 mg/kg
投与経路 i.v.

化学情報

分子量 327.83 化学式

C14H17N3O2S.HCl
CAS No. 105628-07-7 SDF Download Fasudil HCl SDFをダウンロードする
Smiles C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl
保管

In vitro
Batch:

Water : 65 mg/mL

DMSO : 57 mg/mL ( (173.87 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

大学・企業名を記入してください
名前を記入してください
電子メール・アドレスを記入してください 有効なメールアドレスを入力してください
お問い合わせ内容をご入力ください
Tags: Fasudil HClを買う | Fasudil HCl ic50 | Fasudil HCl供給者 | Fasudil HClを購入する | Fasudil HCl費用 | Fasudil HCl生産者 | オーダーFasudil HCl | Fasudil HCl化学構造 | Fasudil HCl分子量 | Fasudil HCl代理店