Fasudil hydrochloride NEW
| Price | $35 | $45 | $68 |
| Package | 50mg | 100mg | 200mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-07 |
Product Details
| Product Name: Fasudil hydrochloride | CAS No.: 105628-07-7 |
| Purity: ≥95% | Supply Ability: 10g |
| Release date: 2024/11/07 |
Product Introduction
Bioactivity
| 名稱 | Fasudil hydrochloride |
| 描述 | Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively. |
| 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. |
| 體外活性 | Intravenous injections of Fasudil at doses of 0.01, 0.03, 0.1, and 0.3 mg/kg decreased mean blood pressure (MBP) and increased heart rate (HR), vertebral blood flow (VBF), cerebral blood flow (CBF), renal blood flow (RBF), and femoral blood flow (FBF) in a dose-dependent manner. A total Fasudil dose of 1.0 ng/mL enhanced cardiac output. Intracoronary injections of 30 μg Fasudil in experimental dogs resulted in approximately a 50% increase in CBF. Oral administration of Fasudil (dose of 100 mg/kg/day) significantly lowered the incidence and average maximum clinical score of experimental autoimmune encephalomyelitis (EAE) in SJL/J mice immunized with PLP p139-151. Fasudil inhibited the proliferation response of mouse spleen cells to antigens, demonstrating cardiovascular protective effects by reducing the activation of JNK and mitigating the mitochondrial translocation of apoptosis-inducing factor (AIF) in ischemic injury. |
| 體內(nèi)活性 | Fasudil induces the disassembly of actomyosin fibers and inhibits cell migration, competitively suppressing Ca2+-induced depolarization and constriction of the rabbit aorta. It blocks contraction responses to KCl, serum phenylalanine, and prostaglandin F2α, and inhibits the proliferation of hepatic stellate cells, formation of stress fibers, and expression of α-SMA, while also repressing cell growth without inducing apoptosis. Fasudil curtails the phosphorylation of ERK1/2, JNK, and p38 MAPK induced by LPA. Additionally, it exerts vasodilatory effects by inhibiting the contraction induced by serotonin, noradrenaline, histamine, angiotensin, and dopamine. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : 32.8 mg/mL (100 mM) DMSO : 60 mg/mL (183.02 mM) |
| 關(guān)鍵字 | Fasudil hydrochloride | TWNT-4 cells | TIMP-1 | HA 1077 | a-SMA | Protein kinase A | Ca channels | PKA | HIV | rat HSCs | AT877 | Rho-associated protein kinase | human HSC | ERK1/2 | Rho-kinase | inhibit | PKC | Ca2+ channels | Rho-associated kinase | HA1077 Hydrochloride | p38 | lysophoaphatidic acid | Fasudil | Ca2+ channel antagonist | JNK | HA 1077 Hydrochloride | Calcium Channel | protein kinases | collagen | LPA | HA1077 | ROCK | Inhibitor | Fasudil Hydrochloride | Protein kinase C | vasodilator | ROK | AT 877 | Human immunodeficiency virus | Autophagy | orally active | HA-1077 Hydrochloride |
| 相關(guān)產(chǎn)品 | Emtricitabine | Hydroxychloroquine | Guanidine hydrochloride |
| 相關(guān)庫 | 疼痛相關(guān)化合物庫 | 經(jīng)典已知活性庫 | 抗病毒庫 | 抗癌上市藥物庫 | 已知活性化合物庫 | TGF-β/Smad靶點(diǎn)化合物庫 | 抗癌藥物庫 |
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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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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