Fasudil (HA-1077) Hydrochloride

製品コードS1573 バッチS157313

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	DMSO	66 mg/mL (201.32 mM)
		Water	66 mg/mL (201.32 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	Rhoキナーゼの強力かつ選択的阻害剤であるFasudil HClは、in vitroアッセイにおいてPKA、PKG、PKC、MLCKに対する阻害能が低く、Ki値はそれぞれ1.6、1.6、3.3、36 μMでした。Fasudilはcalcium channelブロッカーでもあります。
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. Fasudil also exhibits vasodilator actions by inhibition of 5-hydroxytryptamine, noradrenaline, histamine, angiotensin, and dopamine induced spiral strips contraction. Fasudil induces disorganization of actin stress fiber and cell migration inhibition. 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.
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. Fasudil administration displays protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury. 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.

製品説明

Rhoキナーゼの強力かつ選択的阻害剤であるFasudil HClは、in vitroアッセイにおいてPKA、PKG、PKC、MLCKに対する阻害能が低く、Ki値はそれぞれ1.6、1.6、3.3、36 μMでした。Fasudilはcalcium channelブロッカーでもあります。

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.

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

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

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.

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.

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

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.

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

https://pubmed.ncbi.nlm.nih.gov/10454191/
https://pubmed.ncbi.nlm.nih.gov/3598899/
https://pubmed.ncbi.nlm.nih.gov/2611484/

https://pubmed.ncbi.nlm.nih.gov/10448094/
https://pubmed.ncbi.nlm.nih.gov/15998434/
https://pubmed.ncbi.nlm.nih.gov/19061880/
https://pubmed.ncbi.nlm.nih.gov/16996142/

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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：

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The genomic and immunogenomic landscape of mechanics pathway informs clinical prognosis and response to mechanotherapy [ Sci China Life Sci, 2024, 67(8):1549-1562]	PubMed: 39037695
Fasudil Alleviates Postoperative Neurocognitive Disorders in Mice by Downregulating the Surface Expression of α5GABAAR in Hippocampus [ CNS Neurosci Ther, 2024, 30(11):e70098]	PubMed: 39491498
CircPWWP2A promotes renal interstitial fibrosis through modulating miR-182/ROCK1 axis [ Ren Fail, 2024, 46(2):2396455]	PubMed: 39229866
Shroom3-Rock interaction and profibrotic function: Resolving mechanism of an intronic CKD risk allele [ bioRxiv, 2024, 2024.11.22.624409]	PubMed: 39605692
Loss of epigenetic information as a cause of mammalian aging [ Cell, 2023, 186(2):305-326.e27]	PubMed: 36638792
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

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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