Fasudil (HA-1077) HCl
製品コードS1573
分子量(MW)：327.83
Fasudil(HA-1077), 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.
カスタマーフィードバック(4)
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The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
J Clin Invest 2014 124(4), 1646-59. Fasudil (HA-1077) HCl purchased from Selleck.
Tamoxifen was administered to adult Psmc1fl/wt and Psmc1fl/fl Pdgf-Cre-ER mice, followed by treatment with fasudil control (4 and 48 hours after tamoxifen). Representative images of Dylight 488-positive megakaryocytes present in crude bone marrow isolated from Psmc1fl/wt and Psmc1fl/flPdgf-Cre-ER mice immediately after euthanasia. Bone marrow for these studies was isolated from a subset of the mice in A (n=2 per treatment group). Scale bars: 100 um.
J Clin Invest 2014 124(9), 3757-66. Fasudil (HA-1077) HCl purchased from Selleck.
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Effects of GLP-1, fasudil, and H89 on high-glucose (HG)-induced oxidative stress in CMECs. Representative diagram showing dihydroethidine (DHE) staining of CMECs (red, DHE; blue, DAPI; scale bar, 25 um).
Diabetes 2013 62(5), 1697-708. Fasudil (HA-1077) HCl purchased from Selleck.
Representative HE staining of lung section showed that FSD increased pulmonary arteriole wall thickness (orginal magnification ×400).
Pulm Pharmacol Ther, 2018, 50:111-122. Fasudil (HA-1077) HCl purchased from Selleck.
製品安全説明書
ROCK阻害剤の選択性比較
生物活性
| 製品説明 | Fasudil(HA-1077), 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. | |||||||||||||||||||||||||||||||||||||||||||||||||||
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| ターゲット |
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| 体外試験 |
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] |
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| 細胞データ |
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| 体内試験 | 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] |
お薦めの試験操作（参考用のみ）
溶解度 (25°C)
| 体外 | Water | 65 mg/mL (198.27 mM) |
|---|---|---|
| DMSO | 5 mg/mL (15.25 mM) | |
| Ethanol | Insoluble | |
| 体内 |
左から（NMPから）右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ): Saline 混合させたのち直ちに使用することを推奨します。 |
30 mg/mL |
* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。
化学情報
| 分子量 | 327.83 |
|---|---|
| 化学式 | C14H17N3O2S.HCl |
| CAS No. | 105628-07-7 |
| 保管 | 粉 |
| in solvent | |
| 別名 | N/A |
便利ツール
モル濃度計算器
求めたい質量、体積または濃度を計算してください。
質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)
モル濃度計算器方程式
*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA（製品ページで利用可能な）。
希釈計算器
貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます：
開始濃度 x 開始体積 = 最終濃度 x 最終体積
希釈の計算式
この方程式は、一般に略語を使われます：C1V1 = C2V2 ( 入力 出力 )
常に貯蔵液を準備するとき、小びんラベルとMSDS/COA（オンラインで利用できる）で見つかる製品のバッチに特有の分子量を使ってください。
分子量计算器
そのモル質量と元素組成を計算するために、合成物の化学式を入力してください：
チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2
モル濃度計算器
臨床試験
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03391219 | Recruiting | Retinal Vein Occlusion | Shahid Beheshti University of Medical Sciences | January 2018 | Phase 2|Phase 3 |
| NCT03404843 | Completed | Cardiovascular Diseases | Colorado State University | July 14 2017 | Phase 2 |
| NCT01935518 | Unknown status | Amyotrophic Lateral Sclerosis | Peking University Third Hospital | September 2013 | Phase 2 |
| NCT01823081 | Completed | Diabetic Macular Edema | Shahid Beheshti University of Medical Sciences | January 2013 | Phase 3 |
| NCT00670202 | Terminated | Carotid Stenosis | Brigham and Women''s Hospital|Doris Duke Charitable Foundation | March 13 2008 | Phase 2 |
| NCT00498615 | Completed | Raynaud|Scleroderma | Johns Hopkins University | April 2007 | Phase 3 |
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。
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