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1268335-33-6

中文名稱 1,3-DIHYDRO-1-HYDROXY-2,1-BENZOXABOROLE-7-PROPANOIC ACID
英文名稱 1,3-dihydro-1-hydroxy-2,1-Benzoxaborole-7-propanoic acid
CAS 1268335-33-6
分子式 C10H11BO4
分子量 206
MOL 文件 1268335-33-6.mol
1268335-33-6 結(jié)構(gòu)式 1268335-33-6 結(jié)構(gòu)式

基本信息

英文別名
AN3661
1,3-dihydro-1-hydroxy-2,1-Benzoxaborole-7-propanoic acid
3-(1-Hydroxy-1,3-dihydro-2,1-benzoxaborol-7-yl)propanoic acid
3-(1-Hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-7-yl)propanoic acid

物理化學(xué)性質(zhì)

熔點(diǎn)150-151 °C
沸點(diǎn)402.7±55.0 °C(Predicted)
密度1.31±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 250 mg/mL (1213.59 mM)
酸度系數(shù)(pKa)4.52±0.10(Predicted)
形態(tài)Solid
顏色White to off-white

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
1,3-DIHYDRO-1-HYDROXY-2,1-BENZOXABOROLE-7-PROPANOIC ACID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-1282041,3-DIHYDRO-1-HYDROXY-2,1-BENZOXABOROLE-7-PROPANOIC ACID
AN3661
1268335-33-65mg1600元
2024/11/08HY-1282041,3-DIHYDRO-1-HYDROXY-2,1-BENZOXABOROLE-7-PROPANOIC ACID
AN3661
1268335-33-610mM * 1mLin DMSO1760元
2024/11/08HY-1282041,3-DIHYDRO-1-HYDROXY-2,1-BENZOXABOROLE-7-PROPANOIC ACID
AN3661
1268335-33-610mg2600元

常見問題列表

生物活性
AN3661,一種有效的抗瘧疾先導(dǎo)化合物,靶向惡性瘧原蟲的切割和多腺苷酸特異性因子同源物亞基 3 (PfCPSF3)。AN3661 可抑制惡性瘧原蟲實(shí)驗(yàn)室適應(yīng)的菌株(平均 IC50=32 nM),Ugandan 野外分離株 (平均 IC50=64 nM) 和小鼠 P. berghei 和 P. falciparum 的感染。
體外研究

AN3661 is active at nanomolar (IC 50 =20-56?nM) concentrations against P. falciparum laboratory strains known to be sensitive (3D7) or resistant (W2, Dd2, K1, HB3, FCR3 and TM90C2B), and AN3661 is similarly active in ex vivo studies of fresh Ugandan field isolates (mean ex vivo IC 50 =64?nM). AN3661 shows minimal cytotoxicity against mammalian cell lines, with the CC 50 60.5?μM against Jurkat cells, and all other CC 50 values greater than the highest concentrations tested (25?μM or above).
AN3661 inhibits the stability of P. falciparum transcripts.

體內(nèi)研究

AN3661 (50-200 mg.kg; p.o.; daily for 4 days) inhibits murine P. berghei infections with ED 90 (4 days) 0.34 mg/kg.
AN3661 is administered orally for 4 days, beginning on the third day of infection, the ED 90 4 days after initiation of treatment is 0.57?mg/kg.

Animal Model: P. berghei -infected mice (malaria model)
Dosage: 50, 100, 200 mg/kg
Administration: Orally; daily for 4 days
Result: Rapidly controlled parasitemias, with an ED 90 of 0.34?mg/kg. Daily dosages of 50?mg/kg and 100?mg/kg extended survival, and mice treated with 200?mg/kg per day demonstrated long-term cures.
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