| Identification | Back Directory | [Name]
3-Pyridinecarboxamide, N-[(3-aminophenyl)methyl]-6-[4-[(3-fluorophenyl)methoxy]phenoxy]- | [CAS]
838819-70-8 | [Synonyms]
N-(3-Aminobenzyl)-6-(4-((3-fluorobenzyl)oxy)phenoxy)nicotinamide
3-Pyridinecarboxamide, N-[(3-aminophenyl)methyl]-6-[4-[(3-fluorophenyl)methoxy]phenoxy]- | [Molecular Formula]
C26H22FN3O3 | [MOL File]
838819-70-8.mol | [Molecular Weight]
443.47 |
| Chemical Properties | Back Directory | [Boiling point ]
679.4±55.0 °C(Predicted) | [density ]
1.283±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
13.53±0.46(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
YM-244769 is a potent, selective and orally active Na+/Ca2+ exchanger (NCX) inhibitor. YM-244769 preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 can also increase urine volume and urinary excretion of electrolytes in mice[1][2][3]. | [in vivo]
YM-244769 (0.1-1 mg/kg; p.o.; once) exhibits dose-dependently natriuretic action in mice and significantly increases urinary excretion of Ca2+ as well as Ca2+/Cr ratio[2]. | Animal Model: | Wild-type C57BL/6J mice and NCX-KO mice[2] | | Dosage: | 0.1, 0.3 and 1 mg/kg | | Administration: | Oral administration, once | | Result: | Caused a dose-dependent increase (up to approximately 200%) in urine volume and urinary excretion of electrolytes (Na+, K+ and Cl-). Natriuretic actions were equivalently observed in NCX1-KO and WT, but disappeared in NCX2-KO and double KO. |
| [References]
[1] Iwamoto T, Kita S. YM-244769, a novel Na+/Ca2+ exchange inhibitor that preferentially inhibits NCX3, efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. Mol Pharmacol. 2006 Dec;70(6):2075-83. DOI:10.1124/mol.106.028464
[2] Gotoh Y, et al. Genetic knockout and pharmacologic inhibition of NCX2 cause natriuresis and hypercalciuria. Biochem Biophys Res Commun. 2015 Jan 9;456(2):670-5. DOI:10.1016/j.bbrc.2014.12.016
[3] Yamashita K, et al. Inhibitory effect of YM-244769, a novel Na+/Ca2+ exchanger inhibitor on Na+/Ca2+ exchange current in guinea pig cardiac ventricular myocytes. Naunyn Schmiedebergs Arch Pharmacol. 2016 Nov;389(11):1205-1214. DOI:10.1007/s00210-016-1282-y |
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nanjing
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www.linye-e.com/ |
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