| Name | YM758 |
| Description | YM758 is an inhibitor of If current channel. |
| In vitro | 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 vivo | 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 90 mg/mL (191.67 mM), Sonication and heating to 60℃ are recommended.
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| Keywords | YM-758 | YM758 | YM 758 | If channel |
| Inhibitors Related | 8-Pcpt-cGMP sodium | BPU-11 | pan-HCN-IN-1 | Alinidine | Cilobradine hydrochloride | ZD7288 | Zatebradine hydrochloride | 8-Pcpt-cGMP | Ivabradine hydrochloride | RO-275 | KIO-301 chloride | KIO-301 |
| Related Compound Libraries | Bioactive Compound Library | ReFRAME Related Library | Drug Repurposing Compound Library | Inhibitor Library | Clinical Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Ion Channel Targeted Library |
United States
