在線訂購 免費訂購熱線:021-59541103 021-60443211
標(biāo)簽:Vesnarinone (OPC-8212)
聯(lián)系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q: 3004967995
Email:3004967995@qq.com
詳細(xì)地址:上海嘉定區(qū)嘉羅公路1661
化學(xué)性質(zhì):
規(guī)格 | 10mM*1mLinDMSO 5mg 10mg 50mg 100mg |
CAS | 81840-15-5 |
別名 | N/A |
化學(xué)名 | N/A |
分子式 | C22H25N3O4 |
分子量 | 395.45 |
溶解度 | DMSO : 16.67 mg/mL (42.15 mM) |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產(chǎn)品描述:
Vesnarinone is a quinolinone derivative, and its pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux.IC50 value: 1.1 μM (for HERG current)Target: PDE3in vitro: HERG current is inhibited by Vesnarinone with an IC50 of 1.1 μM, whereas KvLQT1/minK current is not significantly depressed by Vesnarinone even at 30 μM. The IC50 value for Vesnarinone inhibition of HERG channels is 1 μM. The IC50 for Vesnarinone inhibition of PDE is reported to be 300 μM. [1] Vesnarinone is a novel cytokine inhibitor, for the treatment of lung fibrosis using a murine model of bleomycin (BLM)-induced pulmonary fibrosis. Vesnarinone inhibits BLM-induced pulmonary fibrosis, at least in part, by the inhibition of acute lung injuries in the early phase. [2] Vesnarinone is a new and novel inotropic drug that has unique and complex mechanisms of action. Vesnarinone inhibits phosphodiesterase, thereby leading to increased intracellular calcium, and also affects numerous myocardial ion channels, resulting in the prolongation of the opening time of sodium channels and the decrease in the delayed outward and inward rectifying potassium current. Vesnarinone has also demonstrated significant effects on cytokine production, which may account for some of its observed clinical benefits.[3] Vesnarinone plays an important role in the regulation of cytokines and suggest that the reduction of cytokine release may contribute to the beneficial effects of the drug in the treatment of heart failure. Vesnarinone inhibits the production of TFN-a and IFN-y by LPS stimulated whole blood from patients with heart failure and from healthy volunteers. [4]in vivo: Vesnarinone reduces the circulating levels of TNF-α. Cumulative evidence showed that a variety of cytokine are involved in the pathogenesis of pulmonary fibrosis
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原創(chuàng)作者:上海莼試生物技術(shù)有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業(yè)部
賬 號:2169 2341 6278