HC-056456 3,4-Bis(2-thienoyl-1,2,5-oxadiazole-N-oxide)|cas:7733-96-2|西域试剂

HC-056456 3,4-Bis(2-thienoyl-1,2,5-oxadiazole-N-oxide),98.89%

产品编号：Bellancom-112729| CAS NO：7733-96-2| 分子式：C₁₂H₆N₂O₄S₂| 分子量：306.32

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-112729	￥900.00	杭州北京（现货）
Bellancom-112729	￥1400.00	杭州北京（现货）
Bellancom-112729	￥2800.00	杭州北京（现货）
Bellancom-112729	￥4800.00	杭州北京（现货）
Bellancom-112729	￥7800.00	杭州北京（现货）

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HC-056456 3,4-Bis(2-thienoyl-1,2,5-oxadiazole-N-oxide)

产品介绍

HC-056456 是一种有效但不完全选择性的 CatSper 通道阻断剂。HC-056456 减慢 [Na⁺]_i 上升，IC₅₀ 为 3 µM。

生物活性

HC-056456 is an effective but not perfectly-selective blocker of CatSper channels. The [Na⁺]_i rise is slowed by HC-056456 (IC₅₀~3 µM).

体外研究

HC-056456 similarly slows the rise of [Ca²⁺]_i that is evoked by alkaline depolarization and reported by fura-2. HC-056456 also selectively and reversibly decreased CatSper currents recorded from patch-clamped sperm. HC-056456 produces a pharmacological phenocopy of the CatSper-null sperm. Acute application of HC-056456 causes rapid loss of flagellar waveform asymmetry from hyperactivated sperm, indicating that continued entry of Ca²⁺ through CatSper channels is required to maintain hyperactivation. HC-056456 selectively and reversibly blocks CatSper currents. The specificity and reversibility of the blockade of CatSper-dependent currents by HC-056456 is examined by using patch clamp recordings. The observed current is blocked slightly more than 50% by 20 µM HC-056456 (estimated IC₅₀ near 15 µM). In concept, it remains possible that CatSper channel heterogeneity explains residual HC-056456-resistant current. The action of HC-056456 on KSper channels, the other major cation channel observed in patch-clamped sperm, is also examined. Subsequent application of 50 µM HC-056456 results in partial blockade of this current. For HC-056456 action on KSper an IC₅₀ near 40 µM is estimated.

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

体内研究

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (408.07 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2646 mL	16.3228 mL	32.6456 mL
5 mM	0.6529 mL	3.2646 mL	6.5291 mL
10 mM	0.3265 mL	1.6323 mL	3.2646 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。-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 (6.79 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.79 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 (6.79 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.79 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。