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64924-67-0

中文名稱 氫溴酸鹵夫酮
英文名稱 Halofuginone hydrobromide
CAS 64924-67-0
分子式 C16H17BrClN3O3.HBr
分子量 495.59
MOL 文件 64924-67-0.mol
更新日期 2024/12/24 16:34:50
64924-67-0 結(jié)構(gòu)式 64924-67-0 結(jié)構(gòu)式

基本信息

中文別名
氫溴酸常山酮
氫溴酸鹵夫酮
常山酮溴酸鹽
鹵夫酮?dú)滗逅猁}
鹵夫酮溴氫酸鹽
氫溴酸溴氯哌喹酮
反式常山酮?dú)滗逅猁}
氫溴酸鹵夫酮 標(biāo)準(zhǔn)品
氫溴酸常山酮/哈洛夫酮
常山酮?dú)滗逅猁}(消旋體)
英文別名
STENOROL
Ru-19110
Tempostatin
RU-19110(HBr)
Unii-ptc2969mv1
55837-20-2 (free)
RU-19110 (hydrobromide)
HALOFUGINONEHYDROBROMIDE
Trans-halofuginone hydrobromide
Halofuginone Hydrobromide 64924-67-0
所屬類別
分析化學(xué):分析標(biāo)準(zhǔn)品

物理化學(xué)性質(zhì)

熔點(diǎn)247° (dec)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度在DMSO中水中的溶解度為至100mM。
形態(tài)neat
顏色White to off-white

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictogramsGHS hazard pictograms
GHS06,GHS09
警示詞危險(xiǎn)
危險(xiǎn)性描述H300+H310+H330-H315-H319-H410
危險(xiǎn)品標(biāo)志Xn
危險(xiǎn)類別碼22
危險(xiǎn)品運(yùn)輸編號(hào)UN2811 - class 6.1 - PG 1 - EHS - Toxic solids, organic, n.o.s., HI: all
WGK Germany3
RTECS號(hào)VA2397066
氫溴酸鹵夫酮價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-N1584A氫溴酸鹵夫酮
Halofuginone hydrobromide
64924-67-05mg1200元
2024/11/08HY-N1584A氫溴酸鹵夫酮
Halofuginone hydrobromide
64924-67-010mM * 1mLin DMSO1320元
2024/11/08HY-N1584A氫溴酸鹵夫酮
Halofuginone hydrobromide
64924-67-010mg1900元

常見問題列表

生物活性
Halofuginone hydrobromide (RU-19110 hydrobromide) 是 Febrifugine 的一種低毒性衍生物,可從 Dichroa febrifuga 中分離出來。Halofuginone 是一種 ATP 競(jìng)爭(zhēng)性的脯氨酰-tRNA 合成酶 (prolyl-tRNA synthetase) 抑制劑,Ki 為 18.3 nM。Halofuginone 是 I 型膠原 (type-I collagen) 合成的特異性抑制劑,并通過抑制 TGF-β 活性可減輕骨關(guān)節(jié)炎。
靶點(diǎn)

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

體外研究

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

Cell Line: KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring the KEAP1 gene mutation
Concentration: 1, 10, 100, 1000, 10000 nM
Incubation Time: 48 hours
Result: The IC 50 s were 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively.

Western Blot Analysis

Cell Line: KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring the KEAP1 gene mutation
Concentration: 1, 10, 100, 1000 nM
Incubation Time: 24 hours
Result: The IC 50 s for NRF2 protein were 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively.
體內(nèi)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.

Animal Model: 3-month-old male C57BL/6J (WT) mice
Dosage: 0.2, 0.5, 1 or 2.5?mg/kg
Administration: Injected intraperitoneally every other day for 1?month
Result: Attenuated progression of OA in ACLT mice.
Animal Model: Male nude mice (BALB/C nu/nu mice) (6-8-week)
Dosage: 0.25 mg/kg
Administration: Intraperitoneally injected; every day; 16 days
Result: The combined treatment with Cisplatin significantly suppressed the tumor volume. NRF2 protein levels in tumors were indeed decreased.
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