4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
产品详情
Senazodan (MCI 154) (hydrochloride) 是一种 Ca2+ 感光剂,同时可抑制 PDE III 的活性。
生物活性
Senazodan (MCI 154) (hydrochloride), as a Ca sensitiser, shows inhibition effect on PDE III.
性状
Solid
IC50 & Target[1][2]
PDE III
体外研究(In Vitro)
Senazodan (hydrochloride) seems to affect directly the actin-myosin crossbridge kinetics, and increases myosin ATPase activity. Senazodan (hydrochloride) produces a concentration-dependent increase in tension development. Senazodan (hydrochloride) enhances Ca binding to myofilaments and to purified cardiac troponin C. Senazodan (hydrochloride) also enhances contractility in guinea-pig papillary muscles by inhibiting PDE III.Senazodan (0.1 nM~0.1 mM) (hydrochloride) shows that the contractile response of superior mesenteric arterie (SMA) to norepinephrine (NE) after hemorrhagic shock is significantly decreased as compared with the normal control group. Senazodan (0.01 mM) (hydrochloride) pretreatment prevents the effects of Ang II, and the concentration-response curve of Ca is shifted to the right as compared with Ang II-alone group.
体内研究(In Vivo)
Senazodan (0.1~2.0 mg/kg; left femoral vein catheterization infusion) (hydrochloride) decreases the pressor effect of norepinephrine (NE).
Senazodan (0.1 mg/kg; i.v.) (hydrochloride) makes LVSP, IP, MC, and Lo all increased significantly, while heart rate is not obviously changed and left ventricular end-diastolic pressure (LVEDP) is reduced remarkably. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Lehtonen LA, et al. Pharmacokinetics and pharmacodynamics of intravenous inotropic agents. Clin Pharmacokinet. 2004;43(3):187-203.[2]. Erhardt L. An emerging role for calcium sensitisation in the treatment of heart failure. Expert Opin Investig Drugs. 2005 Jun;14(6):659-70.[3]. Yang G, et al. Effects of MCI-1
溶解度数据
In Vitro: DMSO : 50 mg/mL (165.15 mM; Need ultrasonic)H2O : 25 mg/mL (82.57 mM; Need ultrasonic)配制储备液