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23256-30-6

中文名稱 硝呋替莫
英文名稱 nifurtimox
CAS 23256-30-6
分子式 C10H13N3O5S
分子量 287.295
MOL 文件 23256-30-6.mol
更新日期 2024/06/20 21:07:20
23256-30-6 結(jié)構(gòu)式 23256-30-6 結(jié)構(gòu)式

基本信息

中文別名
硝呋替莫
NIFURTIMOX [4-氨基-3-甲基四氫-1,4-噻嗪-1,1-二氧化物]
英文別名
Lampit
BAY-2502
NIFURIMOX
Bayer-2502
Bayer 2502
Aids007325
nifurtimox
BAY-A-2502
Aids-007325
nifurtimox USP/EP/BP
所屬類別
生物化工:酶及輔酶類

物理化學(xué)性質(zhì)

熔點(diǎn)177-183°C
沸點(diǎn)550.3±50.0 °C(Predicted)
密度1.4716 (rough estimate)
折射率1.6390 (estimate)
儲(chǔ)存條件Refrigerator
溶解度在DMSO中的溶解度≥13mg/mL
酸度系數(shù)(pKa)-1.01±0.40(Predicted)
形態(tài)粉末
顏色黃色到橙色
水溶解性33g/L(temperature not stated)
BCS Class3
InChIKeyARFHIAQFJWUCFH-IZZDOVSWSA-N

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS08
警示詞警告
危險(xiǎn)性描述H373
防范說明P260-P314-P501
WGK Germany3
毒性LD50 in mice, rats (mg/kg): 3720, 4050 by gavage (Hoffmann)

常見問題列表

應(yīng)用
硝呋替莫是現(xiàn)在幾乎唯一的對(duì)這些病原體具有活性的化合物。該活性可能是基于對(duì)酶Trypanothione還原酶(一種特殊的錐蟲酶)的抑制。這種酶在其他原生動(dòng)物病原體中是不存在的。
作用
硝呋替莫(nifurtimox)是自20世紀(jì)70年代以來治療南美錐蟲?。–hagasdisease)的主要藥物,為一種硝基雜環(huán)類化合物,在細(xì)胞內(nèi)被還原成硝基陰離子自由基、過氧化氫和超氧化物自由基等活性氧(reactiveoxygenspecies,ROS)。硝呋替莫和其他硝基呋喃化合物能夠用于治療癌癥和由血管發(fā)生所介導(dǎo)或引起的疾病或病癥。
生物活性
Nifurtimox (BAY-2502) 是一種抗原蟲劑。
靶點(diǎn)

Trypanosoma cruzi
Lactate dehydrogenase (LDH)

體外研究

Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH). To differentiate if this effect is a result of a reduced LDH activity or a shift in pyruvate metabolism due to activation of PDH, the enzyme activity of LDH is determined after 4 h treatment with 50 μg/mL Nifurtimox. Compared to the untreated control, the LDH activity is significantly reduced for LA-N-1 (P=0.005), IMR-32 (P=0.009), LS (P=0.0035) and SK-N-SH (P=0.0065). Nifurtimox reduces cell viability and induces cell cycle arrest and apoptosis in neuroblastoma cells. To characterize the cytotoxic impacts of Nifurtimox on neuroblastoma, 4 cell lines are subjected to several experiments. Cell viability is reduced for all 4 neuroblastoma cell lines after 24 h incubation with 50 μg/mL to an average of 66%, 63%, 62% and 75% (LA-N-1, IMR-32 LS and SK-N-SH, respectively). The reduction is significant compared to the untreated control (P<0.01) and the vehicle control with DMSO (P<0.05) for all cell lines.

硝呋替莫價(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-W040073硝呋替莫
Nifurtimox
23256-30-65mg800元
2024/11/08HY-W040073硝呋替莫
Nifurtimox
23256-30-610mM * 1mLin DMSO880元
2024/11/08HY-W040073硝呋替莫
Nifurtimox
23256-30-610mg1280元
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