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
- CBNumber:
- CB89636778
- Molecular Formula:
- Molecular Weight:
- 0
- MDL Number:
- MFCD23381171
- MOL File:
- Mol file
YM-244769 dihydrochloride price
YM-244769 dihydrochloride Chemical Properties,Uses,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].
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
YM-244769 dihydrochloride Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9806 | 58 |
Shanghai Chaolan Chemical Technology Center | QQ:65489617 15618227136 | info@SuperLan-chem.com | China | 9945 | 58 |
Jingmo (Xiamen) Biotechnology Co., Ltd | 13621943973 | sales@jamxmpharmatech.com | China | 1105 | 58 |
Beijing Jin Ming Biotechnology Co., Ltd. | 010-60605840 15801484223; | psaitong@jm-bio.com | China | 29778 | 58 |
Bide Pharmatech Ltd. | 400-1647117 13681763483 | product02@bidepharm.com | China | 62163 | 58 |
TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 18779 | 58 |
Suzhou Zhixin Biotechnology Co., Ltd. | 0512-65118909 15162312715 | sales@szzxbio.com | China | 2997 | 58 |
Nanjing Tengyi Biotechnology Co., Ltd | 025-58851786 17714337195 | sales@tybiochem.com | China | 5586 | 58 |