2. Membrane Transporter/Ion Channel
  3. Na+/Ca2+ Exchanger
  4. YM-244769 hydrochloride

YM-244769 hydrochloride 

目录号: HY-107659 纯度: 99.02%
COA 产品使用指南 技术支持

YM-244769 hydrochloride 是一种有效的、选择性的、具有口服活性的 Na+/Ca2+ 交换体 (NCX) 抑制剂。YM-244769 hydrochloride 优先抑制 NCX3，抑制 NCX 单向向外电流 (Ca2+ 进入模式)，IC50 分别为 18 nM 和 50 nM。YM-244769 hydrochloride 可有效预防缺氧/复氧诱导的 SH-SY5Y 神经元细胞损伤。YM-244769 hydrochloride 还能增加小鼠的尿量和尿液中电解质的排泄。

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YM-244769 hydrochloride Chemical Structure

YM-244769 hydrochloride Chemical Structure

CAS No. : 837424-39-2

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规格 价格 是否有货 数量
5 mg ￥1600
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10 mg ￥2600
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25 mg ￥4900
In-stock
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Customer Review

Other Forms of YM-244769 hydrochloride:

YM-244769 hydrochloride 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YM-244769 hydrochloride is a potent, selective and orally active Na+/Ca2+ exchanger (NCX) inhibitor. YM-244769 hydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 hydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 hydrochloride can also increase urine volume and urinary excretion of electrolytes in mice[1][2][3].

IC50 & Target

IC50: 18 nM (NCX3)[1]
体外研究
(In Vitro)

YM-244769 (0.003-1 μM) 剂量依赖性地抑制 NCX1、NCX2 和 NCX3 转染细胞对 45Ca2+ 的初始摄取速率，其 IC50 值分别为 68 、96 和 18 nM[1]。
YM-244769 (0.3 或 1 μM) 可有效保护 SH-SY5Y 细胞和 LLC-PK1 细胞免受缺氧/复氧诱导的乳酸脱氢酶 (LDH) 释放 (1 μM)[1]。
YM-244769 具有反向模式选择性[1]。
YM-244769 (1 和 10 μM) 以浓度和细胞内 [Na+]i 依赖方式抑制 NCX 电流 (INCX)。针对单向外向 NCX 电流 (即钙离子内流模式) 的 IC50 为 0.05 μM。针对双向向外和向内 INCX 的 IC50 值相似，约为 100 nM，Hill 系数约为 1[3]。
YM-244769 对胰蛋白酶不敏感[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

YM-244769 hydrochloride 相关抗体:
体内研究
(In Vivo)

YM-244769 (0.1-1 mg/kg；口服 ；单剂量) 在小鼠中表现出剂量依赖性的利钠作用，并显著增加尿中 Ca2+ 的排泄量以及 Ca2+/肌酐 (Cr) 的比值[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
分子量

479.93

Formula

C26H23ClFN3O3
CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

YM-244769 hydrochloride 相关分类

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  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YM-244769837424-39-2YM244769YM 244769Na+/Ca2+ ExchangerSH-SY5Y cellsneuroprotectivenicotinamideLLC-PK1 cellsNa+/Ca2+ exchangeanti-ischemicNCX3Inhibitorinhibitorinhibit

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