产品
编 号：F504463
分子式：C35H40Cl2N4O6
分子量：683.62
分子式：C35H40Cl2N4O6
分子量：683.62
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
50mg
360
In-stock
100mg
612
In-stock
结构图
CAS No: 89226-75-5
产品详情
生物活性：
Manidipine dihydrochloride is a third-generation, lipophilic, orally active and highly vasoselective calcium channel antagonist (IC50 = 2.6 nM in guinea-pig ventricular cells) and acts as an antihypertensive agent. Manidipine effectively reduces blood pressure as well as improving insulin sensitivity, renal protection, and antiatherosclerotic activity. Manidipine also exerts anti-inflammatory activity mediated by NF-κB and antiviral activity against many flavivirus and negative-strand RNA viruses through the inhibition of calcium channel. Manidipine is widely applied to research of cardiovascular, metabolic disease and infection.
体内研究：
Manidipine dihydrochloride (10 mg/kg, 腹腔注射, b.i.d. 于 4, 5 日) 可延长 SFTSV 感染小鼠的生存期。Manidipine dihydrochloride (25 mg/kg, 腹腔注射, b.i.d. 于前 2 日, 每日一次于后 19 日) 对乙脑病毒感染小鼠有保护作用。Manidipine dihydrochloride (3 mg/kg, 灌胃, 每日一次, 7 d) 可预防异丙肾上腺素诱导的大鼠左心室肥厚。Animal Model:IFNAR-/- mice
Dosage:10 mg/kg
Administration:Intraperitoneal injection (i.p. ), b.i.d. at day 4, day 5
Result:Exhibited a modest, but statistically significant increase in the survival rate of lethal animal model with SFTSV infection, significantly reduced viral titers in the spleen and kidney.
Animal Model:Adult female BALB/c mice (age, 4 weeks)
Dosage:25 mg/kg
Administration:Intraperitoneal injection (i.p. ), b.i.d. for 2 days, then daily for 19 days
Result:Reduced the mortality rate from 73% to 20%, significantly reduced the viral load in infected mice while remarkably alleviated brain damage phenomena. Had little effect on peripheral JEV infection, which indicated that manidipine protected the mice against JEV-induced lethality by decreasing the viral load in the brain.
Animal Model:8-week-old male Wistar rats
Dosage:3 mg/kg
Administration:Intragastric gavage (i.g.), once per day for 7 d
Result:Prevented isoproterenol-induced left ventricular hypertrophy (2.26±0.02 g/kg;p<0.01) as isoproterenol increased left ventricular weight (2.40±0.04 g/kg; p<0.01). Inhibited expression of mRNA of ANP (0.9-fold of the control value; p<0.01), collagen types I (1.1-fold; p<0.01) and type III (1.6-fold; p<0.01), and fibronectin (1.1-fold; p<0.01).
体外研究：
Manidipine dihydrochloride (1 μM, 42 h) 抑制 HUVEC 中脂蛋白诱导的 IL-6 分泌。Manidipine dihydrochloride (1 μM, 16 h) 抑制 10 ng/mL IL-1、10 ng/mL IFN-γ 和 25 ng/mL TNFα 处理的 THP-I 中 IL-6 的分泌。Manidipine dihydrochloride (20 mg/mL, 48/20 h) 抑制 SFTSV (一种负链 RNA 病毒) 在 SW13 细胞中的增殖/基因组复制。Manidipine dihydrochloride (20 mg/mL, 48 h) 干扰 SFTSV N-诱导的包涵体形成。
Manidipine dihydrochloride is a third-generation, lipophilic, orally active and highly vasoselective calcium channel antagonist (IC50 = 2.6 nM in guinea-pig ventricular cells) and acts as an antihypertensive agent. Manidipine effectively reduces blood pressure as well as improving insulin sensitivity, renal protection, and antiatherosclerotic activity. Manidipine also exerts anti-inflammatory activity mediated by NF-κB and antiviral activity against many flavivirus and negative-strand RNA viruses through the inhibition of calcium channel. Manidipine is widely applied to research of cardiovascular, metabolic disease and infection.
体内研究：
Manidipine dihydrochloride (10 mg/kg, 腹腔注射, b.i.d. 于 4, 5 日) 可延长 SFTSV 感染小鼠的生存期。Manidipine dihydrochloride (25 mg/kg, 腹腔注射, b.i.d. 于前 2 日, 每日一次于后 19 日) 对乙脑病毒感染小鼠有保护作用。Manidipine dihydrochloride (3 mg/kg, 灌胃, 每日一次, 7 d) 可预防异丙肾上腺素诱导的大鼠左心室肥厚。Animal Model:IFNAR-/- mice
Dosage:10 mg/kg
Administration:Intraperitoneal injection (i.p. ), b.i.d. at day 4, day 5
Result:Exhibited a modest, but statistically significant increase in the survival rate of lethal animal model with SFTSV infection, significantly reduced viral titers in the spleen and kidney.
Animal Model:Adult female BALB/c mice (age, 4 weeks)
Dosage:25 mg/kg
Administration:Intraperitoneal injection (i.p. ), b.i.d. for 2 days, then daily for 19 days
Result:Reduced the mortality rate from 73% to 20%, significantly reduced the viral load in infected mice while remarkably alleviated brain damage phenomena. Had little effect on peripheral JEV infection, which indicated that manidipine protected the mice against JEV-induced lethality by decreasing the viral load in the brain.
Animal Model:8-week-old male Wistar rats
Dosage:3 mg/kg
Administration:Intragastric gavage (i.g.), once per day for 7 d
Result:Prevented isoproterenol-induced left ventricular hypertrophy (2.26±0.02 g/kg;p<0.01) as isoproterenol increased left ventricular weight (2.40±0.04 g/kg; p<0.01). Inhibited expression of mRNA of ANP (0.9-fold of the control value; p<0.01), collagen types I (1.1-fold; p<0.01) and type III (1.6-fold; p<0.01), and fibronectin (1.1-fold; p<0.01).
体外研究：
Manidipine dihydrochloride (1 μM, 42 h) 抑制 HUVEC 中脂蛋白诱导的 IL-6 分泌。Manidipine dihydrochloride (1 μM, 16 h) 抑制 10 ng/mL IL-1、10 ng/mL IFN-γ 和 25 ng/mL TNFα 处理的 THP-I 中 IL-6 的分泌。Manidipine dihydrochloride (20 mg/mL, 48/20 h) 抑制 SFTSV (一种负链 RNA 病毒) 在 SW13 细胞中的增殖/基因组复制。Manidipine dihydrochloride (20 mg/mL, 48 h) 干扰 SFTSV N-诱导的包涵体形成。
产品资料
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