YM758 是 If 电流通道的抑制剂。

YM758 is an inhibitor of If current channel.

YM758 inhibits rOct1- (IC50 = 23.8 μM) and hOCT1- (IC50 = 40.5 μM) mediated [3H]MPP uptake in a concentration-dependent manner. YM758 inhibits OATP1B1-mediated [3H]E217βG uptake in a concentration-dependent manner(IC50 = 13.0 μM). YM758 shows no inhibitory effect on OATP1B3-mediated [3H]E217βG uptake[1].

In tachycardia-induced dogs, YM758 (0.03, 0.1, and 0.3 mg/kg; i.v.) plasma concentrations rapidly decrease with t1/2s of 1.62, 4.93, and 1.63 h, respectively. The CLtot values are1.71, 1.69, and 1.48 L/h/kg, and Vdss values amount to 3.19, 5.78, and 2.94 L/kg accordingly[2]. The radioactivity in the rat eyeballs after dosing 14C-YM758 is extracted. The radioactivity recovery is 97.1% at 4 h and 67.1% at 24 h. In the eyeball at 4 h after administration, YM758 (the unchanged drug) is the main compound detected (66.7%)[3].

312752-85-5

C26H32FN3O4

469.55

YM758

DMSO:90 mg/mL (191.7mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years