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CAS
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75887-54-6
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中文名称
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蒿乙醚
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英文名称
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β-Arteether
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别名
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(+)-Arteether,Artemotil
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纯度
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HPLC≥98%
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分子式
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C17H28O5
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分子量
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312.4
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外观（性状）
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White to off-white Solid
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储存条件
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Powder : 2-8℃, 2 years; In solvent(母液): -20℃, 1 month; -80℃, 6 months
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溶解性
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Soluble in DMSO
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MDL
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MFCD00869355
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InChIKey
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NLYNIRQVMRLPIQ-XQLAAWPRSA-N
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InChI
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InChI=1S/C17H28O5/c1-5-18-14-11(3)13-7-6-10(2)12-8-9-16(4)20-15(19-14)17(12,13)22-21-16/h10-15H,5-9H2,1-4H3/t10-,11-,12+,13+,14+,15-,16-,17-/m1/s1
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PubChem CID
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3000469
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货期
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1-2天
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SMILES
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C[C@@H]1[C@@](CC[C@@H](C)[C@]2([H])CC[C@]3(C)O4)([H])[C@@]2(OO3)[C@]4([H])O[C@@H]1OCC
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描述
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β-Arteether是青蒿素的半合成类似物(β-Arteether is a semisynthetic analog of artemisinin)
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靶点
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Parasite
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通路
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Anti-infection
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生物活性
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Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant Plasmodium falciparum malaria with an IC50 of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys[1-2].
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IC50
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1.61 nM (Plasmodium falciparum malaria)[1]
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In Vitro
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The antimalarial activity of Artemotil is test in vitro against chloroquine-resistant and chloroquine-sensitive Plasmodium falciparum parasites. The mean 50% inhibitory concentration (IC50) for Artemotil is 1.61 nM (range 1.57-1.92 nM). Artemotil is approximately 2.5-fold more potent than artemisinin[1].
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In Vivo
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Artemotil treatment (25 mg/kg; intravenous injection; daily; for 7 days; Sprague-Dawley male rats) shows anorectic toxicity and causes significant reductions in food consumption and body weight after day 2. AUC on day 7 is 5-fold higher than AUC on day 1. The elimination t1/2 of Artemotil is also prolonged from 13.7 hours (day 1) to 31.2 hours (day 7)[2].
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数据来源文献
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[1]. Shmuklarsky MJ, et al. Comparison of beta-artemether and beta-arteether against malaria parasites in vitro and in vivo. Am J Trop Med Hyg. 1993 Mar;48(3):377-84.
[2]. Li QG, et al. Arteether toxicokinetics and pharmacokinetics in rats after 25 mg/kg/day single and multiple doses. Eur J Drug Metab Pharmacokinet. 1999 Jul-Sep;24(3):213-23.
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规格
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5mg 10mg 20mg
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单位
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瓶
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