Fasudil NEW
| Price | $33 | $45 | $62 |
| Package | 50mg | 100mg | 200mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-06 |
Product Details
| Product Name: Fasudil | CAS No.: 103745-39-7 |
| Purity: 99.84% | Supply Ability: 10g |
| Release date: 2024/11/06 |
Product Introduction
Bioactivity
| 名稱 | Fasudil |
| 描述 | Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK. |
| 激酶實(shí)驗(yàn) | 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°C 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[1]. |
| 體外活性 | Fasudil (Hydrochloride) has vasodilatory action and occupies the adenine pocket of the ATP-binding site of the enzyme[1]. 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]. |
| 體內(nèi)活性 | Fasudil (30 μg) produces an approximate 50% increase in CBF via intra-coronary injection to dogs. 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]. |
| 存儲(chǔ)條件 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : Soluble |
| 關(guān)鍵字 | ROK | Protein kinase C | human HSC | Calcium Channel | Inhibitor | ERK1/2 | vasodilator | Autophagy | inhibit | TIMP-1 | AT 877 | protein kinases | PKC | JNK | rat HSCs | Ca2+ channel antagonist | TWNT-4 cells | Rho-associated protein kinase | orally active | Protein kinase A | Fasudil | p38 | Ca2+ channels | a-SMA | PKA | Ca channels | Rho-kinase | collagen | lysophoaphatidic acid | HA1077 | HA 1077 | Rho-associated kinase | ROCK | AT-877 | LPA |
| 相關(guān)產(chǎn)品 | Stavudine | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Paeonol | Naringin | Gefitinib |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 疼痛相關(guān)化合物庫(kù) | 膜蛋白靶向化合物庫(kù) | 激酶抑制劑庫(kù) | 自噬庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | FDA 上市激酶抑制劑庫(kù) | 已知活性化合物庫(kù) | 離子通道庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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