YM-244769 dihydrochloride
- Product Name
- YM-244769 dihydrochloride
- CAS No.
- 1780390-65-9
- Chemical Name
- YM-244769 dihydrochloride
- Synonyms
- YM244769.HCl;YM-244769 dihydrochloride;N-(3-Aminobenzyl)-6-(4-((3-fluorobenzyl)oxy)phenoxy)nicotinamide dihydrochloride;N-(3-aminobenzyl)-6-(4-((3-fluorobenzyl)oxy)phenoxy)nicotinamide, hydrochloride (1:2);3-Pyridinecarboxamide, N-[(3-aminophenyl)methyl]-6-[4-[(3-fluorophenyl)methoxy]phenoxy]-, hydrochloride (1:2)
- CBNumber
- CB89636778
- Molecular Formula
- C26H24Cl2FN3O3
- Formula Weight
- 0
- MOL File
- Mol file
YM-244769 dihydrochloride Property
- storage temp.
- 4°C, away from moisture
- solubility
- DMSO : 100 mg/mL (193.65 mM; Need ultrasonic)
- form
- Solid
- color
- Off-white to pink
N-Bromosuccinimide Price
- Product number
- SML3362
- Product name
- YM-244769 dihydrochloride
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $87.72
- Updated
- 2025/07/31
- Product number
- SML3362
- Product name
- YM-244769 dihydrochloride
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $412
- Updated
- 2025/07/31
YM-244769 dihydrochloride Chemical Properties,Usage,Production
Uses
YM 244769, is Na+/Ca2+ exchange inhibitor (reverse mode). It can also act as a neuroprotective, that protects against hypoxia/reoxygenation-induced cell damage in neuronal SH-SY5Y cells expressing NCX1 and NCX3.
Biological Activity
YM-244769 dihydrochloride is a potent, selective and orally active Na+/Ca2+ exchanger (NCX) inhibitor. YM-244769 dihydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 dihydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 dihydrochloride can also increase urine volume and urinary excretion of electrolytes in mice[1][2][3]. YM-244769 (0.003-1 μM) inhibits dose dependently the initial rates of 45Ca2+ uptake into NCX1, NCX2, and NCX3 transfectants with IC50 values of 68 ± 2.9, 96 ± 3.5, and 18 ± 1.0 nM, respectively[1].YM-244769 (0.3 or 1 μM) efficiently protects against the hypoxia/reoxygenation-induced lactate dehydrogenase (LDH) release in SH-SY5Y cells and in LLC-PK1 cells (1 μM)[1].YM-244769 possesses reverse mode-selectivity[1].YM-244769 (1 and 10 μM) inhibits NCX current (INCX) in a concentration- and [Na+]i-dependent manner, the IC50 against the unidirectional outward INCX (Ca2+ entry mode) is 0.05 μM. The IC50 values against the bidirectional outward and inward INCX are similar and approximately 100 nM with a Hill coefficient of about 1[3].YM-244769 is trypsin-insensitive[3]. 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].
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. |
storage
Desiccate at RT
References
[1]. Takahiro Iwamoto , et al. 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.[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.[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.
YM-244769 dihydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
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