YM-244769 dihydrochloride|cas:1780390-65-9|西域试剂

YM-244769 dihydrochloride,99.02%

产品编号：Bellancom-136182| CAS NO：1780390-65-9| 分子式：C₂₆H₂₄Cl₂FN₃O₃| 分子量：516.39

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-136182	￥1600.00	杭州北京（现货）
Bellancom-136182	￥2600.00	杭州北京（现货）
Bellancom-136182	￥4900.00	杭州北京（现货）
Bellancom-136182	￥8500.00	杭州北京（现货）
Bellancom-136182	￥15000.00	杭州北京（现货）

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YM-244769 dihydrochloride

产品介绍

YM-244769 dihydrochloride 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 dihydrochloride 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 dihydrochloride 可有效预防缺氧/复氧诱导的 SH-SY5Y 神经元细胞损伤。YM-244769 dihydrochloride 还能增加小鼠的尿量和尿液中电解质的排泄。

生物活性

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.

体外研究

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.
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).
YM-244769 possesses reverse mode-selectivity.
YM-244769 (1 and 10 μM) inhibits NCX current (I_NCX) in a concentration- and [Na⁺]_i-dependent manner, the IC₅₀ against the unidirectional outward I_NCX (Ca²⁺ entry mode) is 0.05 μM. The IC₅₀ values against the bidirectional outward and inward I_NCX are similar and approximately 100 nM with a Hill coefficient of about 1.
YM-244769 is trypsin-insensitive.

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

Cell Viability Assay

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.

体内研究
(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.

西域 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
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.

体内研究

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.

西域 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
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.

体内研究

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.

西域 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
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (193.65 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9365 mL	9.6826 mL	19.3652 mL
5 mM	0.3873 mL	1.9365 mL	3.8730 mL
10 mM	0.1937 mL	0.9683 mL	1.9365 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.03 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.03 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。