中文名 | Dyngo-4a |
英文名 | Dyngo-4a |
别名 | HYDROXY DYNASORE游离 |
英文别名 | Dyng Dyngo-4a DYNGO-4A Dyngo-49 Hydroxy-Dynasore 3-Hydroxy-N′-[(2,4,5-trihydroxyphenyl)methylidene]naphthalene-2-carbohydrazide 3-Hydroxy-2-naphthalenecarboxylic acid 2-[(2,4,5-trihydroxyphenyl)methylene]hydrazide 3-Hydroxynaphthalene-2-carboxylic acid 2-[(2,4,5)-trihydroxyphenyl)methylene]hydrazide 2-Naphthalenecarboxylic acid, 3-hydroxy-, 2-[(2,4,5-trihydroxyphenyl)Methylene]hydrazide |
CAS | 1256493-34-1 |
化学式 | C18H14N2O5 |
分子量 | 338.31 |
密度 | 1.45±0.1 g/cm3(Predicted) |
溶解度 | DMSO: >10 mg/mL |
酸度系数 | 8.28±0.40(Predicted) |
存储条件 | 2-8°C |
外观 | 粉末 |
颜色 | faint yellow to dark yellow |
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 IC 50 values of 2.7 μM and 0.38 μM with or without 0.06% Tween‐80 in the GTPase assay. Hydroxy Dynasore shows an IC 50 of 5.7 μM in clathrin‐mediated endocytosis (CME) assay for inhibition of Tfn‐A594 uptake in U2OS cells. Hydroxy Dynasore shows IC 50 values of 0.38 μM and 1.1 μM in absence of Tween-80, and exhibits IC 50 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 IC 50 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. |
危险品标志 | N - 危害环境的物品 |
风险术语 | 50 - 对水生生物有极高毒性。 |
安全术语 | 61 - 避免释放至环境中。参考特别说明/安全数据说明书。 |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.956 ml | 14.779 ml | 29.559 ml |
5 mM | 0.591 ml | 2.956 ml | 5.912 ml |
10 mM | 0.296 ml | 1.478 ml | 2.956 ml |
5 mM | 0.059 ml | 0.296 ml | 0.591 ml |
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