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Hydroxy-Dynasore
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Hydroxy-Dynasore图片
CAS NO:1256493-34-1
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
Dyngo-4a
产品介绍
Hydroxy Dynasore (Dyngo-4a) 是 Dynasore (HY-15304) 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。
生物活性

Hydroxy Dynasore (Dyngo-4a), a structural analog of Dynasore (HY-15304), is an potency improved, low cytotoxicity and non‐specific bindingdynamininhibitor withIC50 values of 0.38 μM and 2.3 μM for braindynaminI and recombinant ratdynaminII, respectively. Hydroxy Dynasore inhibits dynamin‐dependentendocytosisof transferrin with anIC50of 5.7 μM in vitro.

体外研究
(In Vitro)

Dynamin is a large GTPase enzyme that severs membrane‐ound 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 IC50values of 2.7 μM and 0.38 μM with or without 0.06% Tween‐80 in the GTPase assay[1].
Hydroxy Dynasore shows an IC50of 5.7 μM in clathrin‐mediated endocytosis (CME) assay for inhibition of Tfn‐A594 uptake in U2OS cells[1].
Hydroxy Dynasore shows IC50values of 0.38 μM and 1.1 μM in absence of Tween-80, and exhibits IC50values 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[1].
Hydroxy Dynasore prevents the uptake of BoNT/A-Hc in cultured hippocampal neurons and in motor nerve terminals[2].
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[2].

体内研究
(In Vivo)

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[2].

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

338.31

性状

Solid

Formula

C18H14N2O5

CAS 号

1256493-34-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM2.9559 mL14.7793 mL29.5587 mL
5 mM0.5912 mL2.9559 mL5.9117 mL
10 mM0.2956 mL1.4779 mL2.9559 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
*以上所有助溶剂都可在本网站选购。