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YM-244769 dihydrochloride

CAS No. : 1780390-65-9

MCE 站：YM-244769 dihydrochloride

产品活性：YM-244769 dihydrochloride 是有效的钠钙交换体 (Na⁺/Ca²⁺ exchange; NCX) 抑制剂，YM-244769 dihydrochloride 优先抑制 NCX3 (IC₅₀=18 nM)。YM-244769 dihydrochloride 具有神经和肾脏保护。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Na+/Ca2+ Exchanger

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.
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.
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).

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