DDO-02005 是一种有效的Kv1.5 钙离子通道抑制剂,IC50为 0.72 μM。DDO-02005 在 CaCl2-ACh 房颤大鼠模型中具有良好的抗房颤作用,并能有效抵抗乌头碱引起的心律失常。
产品描述
DDO-02005 is a potent Kv1.5 potassium channel inhibitor with an IC 50 value of 0.72 μM. DDO-02005 has good anti-atrial fibrillation (AF) effect in CaCl 2 -ACh AF rats model and effective anti-arrhythmic activity caused by aconitine [1].
体内活性
DDO-02005 (0.1, 1, 3, 9 mg/kg; IV, single dosage) effectively combat the arrhythmogenic toxicity of aconitine in rats [1]. Pharmacokinetic Parameters of DDO-02005 in Sprague-Dawley rats [1]. IV (1 mg/kg) PO (1.25 mg/kg) t 1/2 (h) 3.23 ± 1.07 6.25 ± 2.40 C max (μg/L) 90.23 ± 28.83 1.27 ± 0.40 AUC 0-t (μg/L·h) 178.42 ± 39.33 4.41 ± 0.69 CL (L/h/kg) 5.83 ± 1.44 36.51 ± 2.54
Cas No.
1186049-44-4
分子式
C21H27Cl2N3O2
分子量
424.36
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years