Hydroxy-Dynasore - CAS:1256493-34-1

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Hydroxy-Dynasore (Synonyms:Dyngo-4a)

目录号 : KM6736 CAS No. : 1256493-34-1 纯度 : 96%

Data Sheet 产品使用指南

Hydroxy Dynasore (Dyngo-4a) 是 Dynasore 结构模拟类似物，是一种改进的，低细胞毒性和通用的 dynamin 抑制剂，针对大脑重组 dynamin I 和重组鼠 dynamin II 的 IC₅₀ 值分别为 0.38 μM 和 2.3μM。Hydroxy Dynasore 抑制 dynamin 依赖性转铁蛋白的内吞作用 (endocytosis) 的 IC₅₀ 为 5.7 μM。

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50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

Hydroxy Dynasore (Dyngo-4a), a structural analog of Dynasore , is an potency improved, low cytotoxicity and non‐specific binding dynamin inhibitor with IC₅₀ values of 0.38 μM and 2.3 μM for brain dynamin I and recombinant rat dynamin II, respectively. Hydroxy Dynasore inhibits dynamin‐dependent endocytosis of transferrin with an IC₅₀ of 5.7 μM in vitro.

体外研究

Dynamin is a large GTPase enzyme that severs membrane‐bound clathrin‐coated vesicles. Endocytosis internalizes portions of cells’ plasma membrane along with extracellular material, is fundamentally important in cell physiology.
Hydroxy Dynasore inhibits Dynamin I (Dyn I) activity with IC₅₀ values of 2.7 μM and 0.38 μM with or without 0.06% Tween‐80 in the GTPase assay.
Hydroxy Dynasore shows an IC₅₀ of 5.7 μM in clathrin‐mediated endocytosis (CME) assay for inhibition of Tfn‐A594 uptake in U2OS cells.
Hydroxy Dynasore shows IC₅₀ values of 0.38 μM and 1.1 μM in absence of Tween-80, and exhibits IC₅₀ values of 4.9 μM and 30.0 μM in presence of Tween-80, respectively. Hydroxy Dynasore is 2.1‐fold selective for DynI versus DynII from Sf21 cells] and DynII (recombinant protein from Sf21 cells) in this GTPase assay.
Hydroxy Dynasore prevents the uptake of BoNT/A-Hc in cultured hippocampal neurons and in motor nerve terminals.
Hydroxy Dynasore (1-100μM; 20 min prior to the addition of Alexa Fluor 488-BoNT/A-Hc) results in depolarization of Hippocampal neurons, it dose-dependently inhibits internalization of Alexa Fluor 488-BoNT/A-Hc with an IC₅₀ of 16.0 ± 1.2 μM.

体内研究

Hydroxy Dynasore (intraperitoneal injection; 30 mg/kg; 1.5-2 h before BoNT/A injection) provides protection again BoNT/A-induced paralysis in the phrenic nerve-hemidiaphragm twitch model in CD-1 mice.

Animal Model:	CD-1 mice.
Dosage:	30 mg/kg
Administration:	Intraperitoneal injection; 1.5–2 h before BoNT/A injection
Result:	Protected BoNT/A-induced paralysis in vivo.

分子式

C₁₈H₁₄N₂O₅

分子量

338.31

CAS号

1256493-34-1

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

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (184.74 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9559 mL	14.7793 mL	29.5587 mL
5 mM	0.5912 mL	2.9559 mL	5.9117 mL
10 mM	0.2956 mL	1.4779 mL	2.9559 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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (6.15 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.15 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 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。