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DDO-02005

Names

[ CAS No. ]:
1186049-44-4

[ Name ]:
DDO-02005

Biological Activity

[Description]:

DDO-02005 is a potent Kv1.5 potassium channel inhibitor with an IC50 value of 0.72 μM. DDO-02005 has good anti-atrial fibrillation (AF) effect in CaCl2-ACh AF rats model and effective anti-arrhythmic activity caused by aconitine[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

[Target]

IC50: 0.72 μM (Kv1.5 potassium channel)[1]


[In Vivo]

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) t1/2 (h) 3.23 ± 1.07 6.25 ± 2.40 Cmax (μg/L) 90.23 ± 28.83 1.27 ± 0.40 AUC0-t (μg/L·h) 178.42 ± 39.33 4.41 ± 0.69 CL (L/h/kg) 5.83 ± 1.44 36.51 ± 2.54

[References]

[1]. Zhao L, et al. Design, synthesis, and biological evaluation of arylmethylpiperidines as Kv1.5 potassium channel inhibitors. J Enzyme Inhib Med Chem. 2022;37(1):462-471.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H27Cl2N3O2

[ Molecular Weight ]:
424.36

Related Compounds