Chemical Structure : YM 758
CAS No.:
312752-86-6
YM 758
(YM758;YM-758)
Catalog No.: PC-60990Not For Human Use, Lab Use Only.
A novel potent "funny" If current channel (If channel) inhibitor that inhibits rOct1- and hOCT1-mediated [3H]MPP uptake with IC50 of 23.8 and 40.5 uM, respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
A novel potent "funny" If current channel (If channel) inhibitor that inhibits rOct1- and hOCT1-mediated [3H]MPP uptake with IC50 of 23.8 and 40.5 uM, respectively; inhibits OATP1B1-mediated [3H]E217βG uptake in HEK293 cells with IC50 of 13.0 uM and has no inhibitory effect on OATP1B3-mediated [3H]E217βG uptake; selectively lowers the heart rate and decreases oxygen consumption by heart muscle.
Physicochemical Properties
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M.Wt
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469.557
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Formula
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C26H32FN3O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20 °C 12 Months; 4°C 6 Months
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- In Solvent
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-80 °C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(-)-N-{2-[(R)-3-(6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline-2-carbonyl)piperidino]ethyl}-4-fluorobenzamide monophosphate
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References
1. Umehara K, et al. Drug Metab Dispos. 2008 Jun;36(6):1030-8.
2. Umehara KI, et al. Xenobiotica. 2008 May;38(5):527-39.
3. Umehara KI, et al. Eur J Drug Metab Pharmacokinet. 2008 Oct-Dec;33(4):211-23.
4. Nakada N. Drugs R D. 2016 Jun;16(2):205-16.
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