YM758 是一个特异性的窦房结 I_f 电流抑制剂。

YM758 is a “funny” I f current channel (I f channel) inhibitor.

Solid

If channel

The inhibitory effect of YM758 on [H]MPP uptake via human/rat organic cation transporters (hOCT1/rOct1) is investigated. YM758 inhibits rOct1- and hOCT1-mediated [H]MPP uptake in a concentration-dependent manner with IC50 values of 23.8 and 40.5 μM, respectively. The IC50 value of YM758 for [C]Metformin uptake via rOct1 may be estimated below 10 μM in the same way, whereas that is much smaller than that for [H]MPP uptake. In addition, the inhibitory effect of YM758 on [H]E217βG uptake via OATP1B1 and OATP1B3 is investigated. YM758 inhibits OATP1B1-mediated [H]E217βG uptake in a concentration-dependent manner with a IC50 value of 13.0 μM. YM758 has no inhibitory effect on OATP1B3-mediated [H]E217βG uptake. has not independently confirmed the accuracy of th

After a single intravenous administration of 0.03, 0.1, and 0.3 mg/kg to tachycardia-induced beagles, YM758 plasma concentrations rapidly decrease with t 1/2 values of 1.62, 4.93, and 1.63 h, respectively. At the corresponding doses, the CL tot values amount to 1.71, 1.69, and 1.48 L/h/kg, and Vd ss values are 3.19, 5.78, and 2.94 L/kg, respectively. Because the plasma concentration 24 h after administration is quantified only in the 0.1 mg/kg dosing group, the larger values of t 1/2 and Vd ss are obtained compared with those in other dosing groups. The PK profile of YM758 in tachycardia-induced dogs appeares to be linear within the dose range of 0.03 to 0.3 mg/kg. The CL tot of YM758 in the blood basis (CL b,dog ) is estimated to be 1.47 to 1.69 L/h/kg. The radioactivity in the rat eyeballs after dosing C-YM

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；In solvent -80°C 6 months

[1]. Umehara K, et al. Hepatic uptake and excretion of (-)-N-{2-[(R)-3-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-2-carbonyl)piperidino]ethyl}-4-fluorobenzamide (YM758), a novel i_f channel inhibitor, in rats and humans. Drug Metab Dispos. 2008 Ju
[2]. Umehara K, et al. Relationship between exposure of (-)-N-{2-[(R)-3-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-2-carbonyl)piperidino]ethyl}-4-fluorobenzamide (YM758), a "funny" i_f current channel inhibitor, and heart rate reduction in tachyca

In Vitro: DMSO : 100 mg/mL (212.97 mM; ultrasonic and warming and heat to 60°C)配制储备液