氢溴酸卤夫酮 CAS#: 64924-67-0

微信扫码

氢溴酸卤夫酮

生物活性靶点体外研究体内研究 用途与合成方法 MSDS 氢溴酸卤夫酮价格(试剂级) 上下游产品信息

中文名称	氢溴酸卤夫酮
中文同义词	氢溴酸常山酮溶液, 100PPM;氢溴酸常山酮/哈洛夫酮;卤夫酮氢溴酸盐;-溴-6-氯-3-[3-(3-羟基-2-哌啶基)-2-丙酮基]-4(3H)-喹唑啉酮氢溴酸盐;7-溴-6-氯-3-[3-(3-羟基-2-哌啶基)-2-丙酮基]-4(3H)-喹唑啉酮氢溴酸盐;氢溴酸卤夫酮;氢溴酸溴氯哌喹酮;氢溴酸常山酮
英文名称	Halofuginone hydrobromide
英文同义词	Ru-19110;Tempostatin;Unii-ptc2969mv1;rel-7-BroMo-6-chloro-3-[3-[(2R,3S)-3-hydroxy-2-piperidinyl]-2-oxopropyl]-4(3H)-quinazolinone  HydrobroMide;trans-(+/-)-7-BroMo-6-chloro-3-[3-(3-hydroxy-2- piperidinyl)-2-oxopropyl]-4(3H)-quinazolinone MonohydrobroMide;7-BroMo-6-chloro-3-(3-((2S,3R)-3-hydroxypiperidin-2-yl)-2-oxopropyl)quinazolin-4(3H)-one hydrobroMide;HALOFUGINONEHYDROBROMIDE;STENOROL
CAS号	64924-67-0
分子式	C16H17BrClN3O3.HBr
分子量	495.59
EINECS号
相关类别	其他兽药标准品;化工中间体;原料药;原料药;有机化工原料;标准品;Amines;Chiral Reagents;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals
Mol文件	64924-67-0.mol
结构式

氢溴酸卤夫酮 性质

氢溴酸卤夫酮 用途与合成方法

生物活性

Halofuginone hydrobromide (RU-19110 hydrobromide) 是 Febrifugine 的一种低毒性衍生物，可从 Dichroa febrifuga 中分离出来。Halofuginone 是一种 ATP 竞争性的脯氨酰-tRNA 合成酶 (prolyl-tRNA synthetase) 抑制剂，Ki 为 18.3 nM。Halofuginone 是 I 型胶原 (type-I collagen) 合成的特异性抑制剂，并通过抑制 TGF-β 活性可减轻骨关节炎。

靶点

Ki: 18.3±0.5 nM (prolyl-tRNA synthetase)

体外研究

Halofuginone competitively inhibits prolyl-tRNA synthetase by occupying both the prolineand tRNA-binding pockets of prolyl-tRNA synthetase.  
 The IC     ₅₀    s of Halofuginone (1, 10, 100, 1000, 10000 nM; 48 hours) are 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively.  
 The IC     ₅₀    s of Halofuginone (1, 10, 100, 1000 nM; 24 hours) for NRF2 protein are 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively. The IC     ₅₀    of Halofuginone for global protein synthesis is 22.6 and 45.7 nM in KYSE70 and A549 cells, respectively.  

Cell Viability Assay

Western Blot Analysis

体内研究

Halofuginone (0.2, 0.5, 1 or 2.5 mg/kg; injected intraperitoneally every other day for 1 month) attenuates progression of OA in anterior cruciate ligament transection (ACLT) mice. Lower concentration (0.2 or 0.5 mg/kg) has minimal effects on subchondral bone and higher concentration (2.5 mg/kg) induces proteoglycan loss in articular cartilage.  
 Halofuginone (0.25 mg/kg; intraperitoneally injected; every day; 16 days) decreases NRF2 protein levels in tumors. While the tumor volumes do not change substantially between treatments with the vehicle, Halofuginone (0.25 mg/kg, intraperitoneally injected, every day) or cisplatin alone. Combined treatment with Halofuginone and Cisplatin significantly suppresses the tumor volume compared to treatment with Halofuginone or cisplatin alone.  

安全信息

MSDS信息

氢溴酸卤夫酮 价格(试剂级)

氢溴酸卤夫酮 上下游产品信息