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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
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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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML3362
Product name
YM-244769 dihydrochloride
Purity
≥98% (HPLC)
Packaging
5MG
Price
$87.72
Updated
2025/07/31
Sigma-Aldrich
Product number
SML3362
Product name
YM-244769 dihydrochloride
Purity
≥98% (HPLC)
Packaging
25MG
Price
$412
Updated
2025/07/31
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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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YM-244769 dihydrochloride Suppliers

Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
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58
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
71826
Advantage
60
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ:65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
Country
China
ProdList
9119
Advantage
58
Jingmo (Xiamen) Biotechnology Co., Ltd
Tel
13621943973; 13621943973
Email
sales@jamxmpharmatech.com
Country
China
ProdList
1168
Advantage
58
Beijing Jin Ming Biotechnology Co., Ltd.
Tel
010-60605840 15801484223;
Email
psaitong@jm-bio.com
Country
China
ProdList
29757
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58
Bide Pharmatech Ltd.
Tel
400-1647117 13681763483
Email
product02@bidepharm.com
Country
China
ProdList
62220
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58
TargetMol Chemicals Inc.
Tel
4008200310
Email
marketing@tsbiochem.com
Country
China
ProdList
24961
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58
Shanghai Maclean Biochemical Technology Co., LTD
Tel
021-021-50706066 15221275939
Email
shenlinxing@macklin.cn
Country
China
ProdList
29784
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58
Suzhou Zhixin Biotechnology Co., Ltd.
Tel
0512-65118909 18100677375
Email
sales@szzxbio.com
Country
China
ProdList
2993
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58
Shanghai Jieshikai Biotechnology Co. , Ltd.
Tel
021-57520305 13795461237
Email
zhuruyan@jskchem.com
Country
China
ProdList
49234
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58

1780390-65-9, YM-244769 dihydrochlorideRelated Search:


  • YM-244769 dihydrochloride
  • YM244769.HCl
  • N-(3-Aminobenzyl)-6-(4-((3-fluorobenzyl)oxy)phenoxy)nicotinamide dihydrochloride
  • 3-Pyridinecarboxamide, N-[(3-aminophenyl)methyl]-6-[4-[(3-fluorophenyl)methoxy]phenoxy]-, hydrochloride (1:2)
  • N-(3-aminobenzyl)-6-(4-((3-fluorobenzyl)oxy)phenoxy)nicotinamide, hydrochloride (1:2)
  • 1780390-65-9