Antibodies
Fasudil (HA-1077) HCl
- 貨號 Cat. No.
- S1573
- 規格 Size
- 10mM/1mLã€200mgã€500mg
- 品牌 Brand
- Selleckchem
Description
Fasudil (HA-1077) HCl
Catalog No.S15732 Product Citations
Fasudil (HA-1077) is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM, respectively.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | Fasudil (HA-1077) is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM, respectively. | |||||
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| Targets | ROCK-II | PKA | PKG | PKC | MLCK | |
| IC50 | 0.33 μM (Ki) | 1.6 μM (Ki) | 1.6 μM (Ki) | 3.3 μM (Ki) | 36 μM (Ki) [1] | |
| 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] | |||||
| 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] | |||||
| Features | ||||||
Protocol(Only for Reference)
Kinase Assay: [1]
| 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. |
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References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00498615 | Completed | Raynaud|Scleroderma | Johns Hopkins University | 2007-08 | Phase 3 |
| NCT00670202 | Recruiting | Carotid Stenosis | Brigham and Women’s Hospital|Doris Duke Charitable Foundation | 2008-08 | Phase 2 |
| NCT01069042 | Recruiting | Heart Failure | National Cheng-Kung University Hospital | 2010-02 | Phase 4 |
| NCT01823081 | Recruiting | Diabetic Macular Edema | Shahid Beheshti Medical University | 2013-01 | Phase 3 |
| NCT01935518 | Recruiting | Amyotrophic Lateral Sclerosis | Peking University Third Hospital | 2013-09 | Phase 2 |
Chemical Information
Download Fasudil (HA-1077) HCl SDF
| Molecular Weight (MW) | 327.83 |
|---|---|
| Formula | C14H17N3O2S.HCl |
| CAS No. | 105628-07-7 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | AT-877 |
| Solubility (25°C) * | In vitro | DMSO | 5 mg/mL (15 mM) |
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| Water | 66 mg/mL (201 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | Saline, | 30 mg/mL | |
| * <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. | |||
| Chemical Name | 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline hydrochloride |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.32783 | 3.2783 | - | - |
Product Citations (2)
Glucagon-like peptide-1 protects against cardiac microvascular injury in diabetes via a cAMP/PKA/Rho-dependent mechanism. [Wang D, et al. Diabetes 2013;62(5):1697-708]
Correlation between platelet-derived growth factor signaling pathway and inflammation in desoxycorticosterone-induced salt-sensitive hypertensive rats with myocardial fibrosis. [Fan B, et al. Int J Clin Exp Pathol 2013;6(11):2468-75]
