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1256493-34-1

中文名稱 DYNGO-4A
英文名稱 2-Naphthalenecarboxylic acid, 3-hydroxy-, 2-[(2,4,5-trihydroxyphenyl)Methylene]hydrazide
CAS 1256493-34-1
分子式 C18H14N2O5
分子量 338.31
MOL 文件 1256493-34-1.mol
更新日期 2024/12/15 19:35:15
1256493-34-1 結(jié)構(gòu)式 1256493-34-1 結(jié)構(gòu)式

基本信息

中文別名
化合物DYNGO-4A
DYNGO?4A,新型的動(dòng)力抑制劑
HYDROXY DYNASORE游離
3-羥基-N′-((2,4,5-三羥基苯基)亞甲基)-2-萘酰肼
英文別名
o-4a
Dyng
Dyngo-49
Dyngo-4a
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
所屬類別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

密度1.45±0.1 g/cm3(Predicted)
儲(chǔ)存條件2-8°C
溶解度二甲基亞砜:>10mg/mL
酸度系數(shù)(pKa)8.28±0.40(Predicted)
形態(tài)粉末
顏色淡黃色至深黃色

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictogramsGHS hazard pictogramsGHS hazard pictograms
GHS07,GHS08,GHS09
警示詞危險(xiǎn)
危險(xiǎn)性描述H302-H361-H372-H410
危險(xiǎn)品標(biāo)志N
危險(xiǎn)類別碼50
安全說(shuō)明61
WGK Germany3

常見(jiàn)問(wèn)題列表

生物活性
Hydroxy Dynasore (Dyngo-4a) 是 Dynasore (HY-15304) 結(jié)構(gòu)模擬類似物,是一種改進(jìn)的,低細(xì)胞毒性和通用的 dynamin 抑制劑,針對(duì)大腦重組 dynamin I 和重組鼠 dynamin II 的 IC50 值分別為 0.38 μM 和 2.3μM。Hydroxy Dynasore 抑制 dynamin 依賴性轉(zhuǎn)鐵蛋白的內(nèi)吞作用 (endocytosis) 的 IC50 為 5.7 μM。
體外研究

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.

體內(nèi)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.
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