Fasudil HCl

製品コードS1573 バッチS157311

化学情報

	Synonyms	AT-877,HA-1077 HCl	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₄H₁₇N₃O₂S.HCl
	分子量	327.83	CAS No.	105628-07-7
Solubility (25°C)*	体外	Water	65 mg/mL (198.27 mM)
		DMSO	57 mg/mL (173.87 mM)
		Ethanol	Insoluble
* <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	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.
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]

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.

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]

プロトコル(参考用のみ)

キナーゼアッセイ	Cyclic AMP-dependent protein kinase activity assay
キナーゼアッセイ	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.
細胞アッセイ	細胞株	Cell-free assays
	濃度	Ki values of 1.6 and 36 µM for cyclic nucleotide-dependent protein kinases and Ca2+/calmodulin-dependent myosin light chain kinase, respectively.
	反応時間
	実験の流れ
動物実験	動物モデル	Mongrel dogs
	投薬量	0.01, 0.03, 0.1 and 0.3 mg/kg
	投与方法	i.v.

参考

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カスタマーフィードバック

: Data from [J Clin Invest, 2014, 124(4), 1646-59]

: Data from [Data independently produced by J Clin Invest, 2014, 124(9), 3757-66]

: Data from [Data independently produced by Diabetes, 2013, 62(5), 1697-708]

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：

Fasudil may alleviate alcohol-induced astrocyte damage by modifying lipid metabolism, as determined by metabonomics analysis [ PeerJ, 2023, 11:e15494]	PubMed: 37304877
Inhibition of the Rho/ROCK pathway promotes the expression of developmental and migration-related genes in astrocytes exposed to alcohol [ Alcohol, 2023, 115:5-12]	PubMed: 37481044
A rare non-coding enhancer variant in SCN5A contributes to the high prevalence of Brugada syndrome in Thailand [ medRxiv, 2023, 10.1101/2023.12.19.23299785]	PubMed: none
Acquired temozolomide resistance in MGMTlow gliomas is associated with regulation of homologous recombination repair by ROCK2 [ Cell Death Dis, 2022, 13(2):138]	PubMed: 35145081
Rho-Kinase Inhibition Improves the Outcome of Focal Subcortical White Matter Lesions [ Stroke, 2022, 53(7):2369-2376]	PubMed: 35656825
Arolein, an endogenous aldehyde induces synaptic dysfunction in vitro and in vivo: Involvement of RhoA/ROCK2 pathway [ Aging Cell, 2022, e13587]	PubMed: 35315217
AURKA and PLK1 inhibition selectively and synergistically block cell cycle progression in diffuse midline glioma [ iScience, 2022, 25(6):104398]	PubMed: 35637734
Amyloid-β Induces Cdh1-Mediated Rock2 Stabilization Causing Neurodegeneration [ Front Pharmacol, 2022, 13:884470]	PubMed: 35496276
Involvement of Paired Immunoglobulin-Like Receptor B in Cognitive Dysfunction Through Hippocampal-Dependent Synaptic Plasticity Impairments in Mice Subjected to Chronic Sleep Restriction [ Mol Neurobiol, 2022, 10.1007/s12035-022-03127-4]	PubMed: 36417104
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7]	PubMed: 34997030

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。

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