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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
4°C, sealed storage, away from moisture
- 英文名：
RU-19110 hydrobromide
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
64924-67-0
- 规格：
10 mM * 1 mL/5 mg/10 mg/25 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1320.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥1200.0 |
| 规格： | 10 mg | 产品价格： | ￥1900.0 |
| 规格： | 25 mg | 产品价格： | ￥2900.0 |
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Halofuginone hydrobromide
CAS No. : 64924-67-0
MCE 国际站：Halofuginone hydrobromide
产品活性：Halofuginone (RU-19110) hydrobromid，Febrifugine 的衍生物，是一种竞争性的脯氨酰-tRNA 合成酶 (prolyl-tRNA synthetase) 抑制剂，Ki 为 18.3 nM。Halofuginone hydrobromid 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。Halofuginone hydrobromid 也是一种有效的肺血管扩张剂，可激活 Kv 通道并阻断电压门控、受体操作和存储操作的 Ca2+ channels 通道。Halofuginone hydrobromid 具有抗疟疾、抗炎、抗癌、抗纤维化作用。
研究领域：Cell Cycle/DNA Damage | TGF-beta/Smad | Stem Cell/Wnt | Anti-infection | Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点：DNA/RNA Synthesis | TGF-beta/Smad | Parasite | Sodium Channel | Calcium Channel
In Vitro: Halofuginone competitively inhibits prolyl-tRNA synthetase by occupying both the prolineand tRNA-binding pockets of prolyl-tRNA synthetase.
The IC50s of Halofuginone (1, 10, 100, 1000, 10000 nM; 48 hours) are 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively.
The IC50s 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 IC50 of Halofuginone for global protein synthesis is 22.6 and 45.7 nM in KYSE70 and A549 cells, respectively.
Halofuginone increases voltage-gated K+ (Kv) currents in pulmonary artery smooth muscle cells (PASMC) and K+ currents through KCNA5 channels in HEK cells transfected with KCNA5 gene. Halofuginone (0.03-1μM) inhibits receptor-operated Ca2+ entry (ROCE) in HEK cells transfected with calcium-sensing receptor gene and attenuated store-operated (SOCE) Ca2+ entry in PASMC.
In Vivo: 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.
Intraperitoneal administration of Halofuginone (0.3mg/kg, for 2 weeks) partially reverses the established pulmonary hypertension in mice.
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文献和实验β-aminoethylisothiuronium bromide hydrobromide或S-（2-aminoethyl）isothiuro-nium bromide hydrobromide的略称。分子式为C 3 H 11 Br 2 N 3 S，分子量为281.04。1955年美国的多尔蒂和伯内特（D．G．Doherty和W．T．Burnett）提出了它对大白鼠具有辐射防护作用的报告，从而成为出名的显效物质的例子。由于AET在近中性的水溶液中
成分是莨菪碱，所含生物碱按莨菪碱计算应为1%）。口服1～2片/次，3次/日。 氢溴酸山莨菪碱（anisodamine hydrobromide）口服，5～10mg/次，3次/日。静脉注射或肌内注射，5～10mg/次，1～2次/日。 氢溴酸东莨菪碱（scopolamine hydrobromide）口服，0.2～0.3mg/次，3次/日。皮下或肌内注射，0.2～0.5mg/次。极量：口服，0.6mg/次，2mg/日；注射0.5mg/次，1.5mg/日 氢溴
mg(颠茄浸膏的主要成分是莨菪碱，所含生物碱按莨菪碱计算应为1%）。口服1～2片/次，3次/日。 氢溴酸山莨菪碱（anisodamine hydrobromide）口服，5～10mg/次，3次/日。静脉注射或肌内注射，5～10mg/次，1～2次/日。 氢溴酸东莨菪碱（scopolamine hydrobromide）口服，0.2～0.3mg/次，3次/日。皮下或肌内注射，0.2～0.5mg/次。极量：口服，0.6mg/次，2mg/日；注射0.5mg/次，1.5mg/日 氢溴
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