Fasudil (HA-1077) HCl |
カタログ番号GC14289 |
Fasudil(HA-1077; AT877)塩酸塩は非特異的RHOA/ROCK阻害剤であり、0.33 ############788787878788788788878878887###8年にかうしたタンパク質キナーゼにも阻害効果があります。 offlineefficient_models_2022q2.md;M, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively.en_ja_2022q2.mdFasudil (HA-1077) HCl is also a potent Ca2+ channel antagonist and vasodilator.en_ja_2022q2.md
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 105628-07-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines |
5637, UM-UC-3 and SCC-4 cell lines |
Preparation method |
The solubility of this compound in DMSO is >16.4 mg/ml. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition |
0-30 μM |
Applications |
Lysophosphatidic acid and geranylgeraniol induced an increase of cell proliferation and migration in association with promotion of RhoA activity and upregulation of ROCK expression. Fasudil (HA-1077) could suppress cell proliferation and migration, and also induce apoptosis in a dose-dependent manner. Fasudil (HA-1077) also dramatically suppressed the expression of ROCK-I and ROCK-II, but did not affect RhoA activity. |
Animal experiment [2]: | |
Animal models |
Cbl/Cbl-b deficiency-driven murine model of myeloproliferative disorders |
Dosage form |
100 mg/kg daily by oral gavage |
Application |
In the Cbl/Cbl-b deficiency-driven murine model of myeloproliferative disorders, by 2 weeks of treatment, total white cell and monocyte counts were significantly lower in mice treated with fasudil. A trend towards improved survival in fasudil-treated mice that did not reach statistical significance was also observed. Notably, prolonged survival beyond 27 weeks was seen in two fasudil-treated mice, nearly twice the 16-week average life-span in the Cbl/Cbl-b DKO MPD model. |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Abe, H., et al., The Rho-kinase inhibitor HA-1077 suppresses proliferation/migration and induces apoptosis of urothelial cancer cells. BMC Cancer, 2014. 14: p. 412. [2] William, B.M., et al., Fasudil, a clinically safe ROCK inhibitor, decreases disease burden in a Cbl/Cbl-b deficiency-driven murine model of myeloproliferative disorders. Hematology, 2015. |
Fasudil (HA-1077) HCl is a selective inhibitor of ROCK with IC50 value of 0.74 μM [1].
Rho-associated protein kinase (ROCK) belongs to the AGC family of serine-threonine kinases and plays a pivotal role in regulating a variety of cellular processes. It has been reported that abnormal expression of ROCK is correlated with numerous diseases and infections [2].
Fasudil (HA-1077) HCl is a potent ROCK inhibitor and has a different structure with the reported ROCK inhibitor Y-27632. When tested with 2 human bladder cancer cell lines (5637 and UM-UC-3), Fasudil (HA-1077) HCl treatment inhibits cell proliferation, decreases cell migration and induced cell apoptosis in a dose dependent manner via blocking Rho/ROCK pathway [3]. In oral squmous cell carcinoma SCC-4 cells, administration of Fasudil (HA-1077) HCl markedly decreases cell motility and inhibits cell migration or invasion in a dose dependent manner (1, 50 and 100 μmol/L [4].
In the Cbl/Cbl-b deficiency-driven murine model of myeloproliferative disorders, oral administration of Fasudil (HA-1077) HCl (100 mg/kg, daily) markedly increases the total white cell and monocyte numbers while prolonged survival time has trend but no statistical difference compared with the control group [2].
References:
[1]. Wickman, G., C. Lan, and B. Vollrath, Functional roles of the rho/rho kinase pathway and protein kinase C in the regulation of cerebrovascular constriction mediated by hemoglobin: relevance to subarachnoid hemorrhage and vasospasm. Circ Res, 2003. 92(7): p. 809-16.
[2]. William, B.M., et al., Fasudil, a clinically safe ROCK inhibitor, decreases disease burden in a Cbl/Cbl-b deficiency-driven murine model of myeloproliferative disorders. Hematology, 2015.
[3]. Abe, H., et al., The Rho-kinase inhibitor HA-1077 suppresses proliferation/migration and induces apoptosis of urothelial cancer cells. BMC Cancer, 2014. 14: p. 412.
[4]. Moreira Carboni, S.S., et al., HA-1077 inhibits cell migration/invasion of oral squamous cell carcinoma. Anticancer Drugs, 2015.
Cas No. | 105628-07-7 | SDF | |
Chemical Name | 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline;hydrochloride | ||
Canonical SMILES | C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl | ||
Formula | C14H17N3O2S.HCl | M.Wt | 327.83 |
溶解度 | ≥ 16.4mg/mL in DMSO, ≥ 4.81 mg/mL in EtOH with ultrasonic, ≥ 50 mg/mL in Water | Storage | Store at 4°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.0504 mL | 15.2518 mL | 30.5036 mL |
5 mM | 0.6101 mL | 3.0504 mL | 6.1007 mL |
10 mM | 0.305 mL | 1.5252 mL | 3.0504 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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