Name | YM-244769 dihydrochloride |
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Description | YM-244769 dihydrochloride is a potent Na+/Ca2+ exchange (NCX) inhibitor that preferentially inhibits NCX3 (IC50=18 nM). Neuronal and renal protection[1]. |
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Related Catalog | |
In Vitro | YM-244769 preferentially inhibits intracellular Na+-dependent 45Ca2+ uptake via NCX3 (IC50=18 nM); the inhibition is 3.8- to 5.3-fold greater than for the uptake via NCX1 or NCX2, but it does not significantly affect extracellular Na+-dependent 45Ca2+ efflux via NCX isoforms[1]. 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, indicating that YM-244769 is approximately four to five times more selective to NCX3 than other isoforms[1]. YM-244769 (0.3 or 1 μM) efficiently suppresses the hypoxia/reoxygenation-induced cell damage in SH-SY5Y cells treated with NCX1 antisense (i.e., SH-SY5Y cells primarily expressing NCX3) more than in those treated with NCX3 antisense (i.e., SH-SY5Y cells primarily expressing NCX1)[1]. Cell Viability Assay[1] Cell Line: SH-SY5Y cells treated with NCX1 or NCX3 antisense Concentration: 0.3 and 1 μM Incubation Time: Result: Hypoxia/reoxygenation-induced LDH release was significantly attenuated: reduction in cell damage was greater in cells treated with NCX3 antisense (by 61%) than in cells treated with NCX1 antisense (by 35%). 0.3 or 1 μM efficiently suppressed the hypoxia/reoxygenation-induced cell damage in SH-SY5Y cells treated with NCX1 antisense more than in those treated with NCX3 antisense. |
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Molecular Formula | C26H24Cl2FN3O3 |
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Molecular Weight | 516.39 |
Hazard Codes | Xi |
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