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YM758 is an inhibitor of If current channel.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $46 | In Stock | |
5 mg | $137 | In Stock | |
10 mg | $223 | In Stock | |
25 mg | $369 | In Stock | |
50 mg | $521 | In Stock | |
100 mg | $702 | In Stock | |
200 mg | $947 | In Stock | |
1 mL x 10 mM (in DMSO) | $143 | In Stock |
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]. |
Molecular Weight | 469.55 |
Formula | C26H32FN3O4 |
Cas No. | 312752-85-5 |
Smiles | COc1cc2CCN(Cc2cc1OC)C(=O)[C@@H]1CCCN(CCNC(=O)c2ccc(F)cc2)C1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 90 mg/mL (191.7 mM), Sonication and heating to 60℃ are recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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