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YM 758

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

M.Wt 469.557
Formula C26H32FN3O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(-)-N-{2-[(R)-3-(6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline-2-carbonyl)piperidino]ethyl}-4-fluorobenzamide monophosphate

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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