Zatebradine

Research use only, not for human use.

Zatebradine (UL-FS49) is a potent blocker (antagonist) of hyperpolarization-activated cyclic nucleotide-gated (HCN) channel, a specific bradycardic agent.

Zatebradine (UL-FS49) is a potent blocker (antagonist) of hyperpolarization-activated cyclic nucleotide-gated (HCN) channel, a specific bradycardic agent; blocks cardiac pacemaker current (If), decreases the rate of spontaneously beating guinea-pig atria with EC50 of 0.030 ug/mL.Heart Failure Discontinued.

The use-dependent blockade by Zatebradine of the cardiac pacemaker current from rabbit sino-atrial node cells has an apparent Kd of 480 nM.

Zatebradine (0-20 mg/kg; intraperitoneal injection; for 30 minutes; male C57/Bl6-mice) reduces the heart rate dose-dependently from 600 to 200 bpm with ED50 value of 1.8 mg/kg and induces increasing arrhythmia. Animal Model:Male C57/Bl6-mice Dosage:0 mg/kg, 0.1 mg/kg, 1 mg/kg, 10 mg/kg, 20 mg/kg Administration:Intraperitoneal injection; for 30 minutes Result:Observed acute blood glucose reduction, dose-dependently reduced glycated hemoglobin, significantly prevented the decrease of IRI levels at doses of 3 and 10 mg/kg, and no difference in food intake or body weight.

UL-FS49

Membrane Transporter/Ion Channel

HCN Channel

HCN Channel

Cardiovascular Disease

——

85175-67-3

456.5744

C26H36N2O5

>98% (HPLC)

10 mM in DMSO

CN(CCCN1CCC2=CC(=C(C=C2CC1=O)OC)OC)CCC3=CC(=C(C=C3)OC)OC

2H-3-Benzazepin-2-one, 3-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-

(-20℃)

With Ice Pack

≥ 2 years