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103337-74-2
  • names:

    Letrazuril

  • CAS号:

    103337-74-2

    MDL Number: MFCD00867212
  • MF(分子式): C17H9Cl2FN4O2 MW(分子量): 391.18
  • EINECS:No data available Reaxys Number:No data available
  • Pubchem ID:59745 Brand:BIOFOUNT
来曲珠利
来曲珠利(103337-74-2,Letrazuril)是一种抗艾滋病毒的化合物。Letrazuril已用于研究治疗HIV感染和隐孢子虫病的试验中。
货品编码 规格 纯度 价格 (¥) 现价(¥) 特价(¥) 库存描述 数量 总计 (¥)
YZM000672-5mg 5mg 98.27% ¥ 3543.00 ¥ 3543.00 2-3天
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¥ 0.00
YZM000672-1mg 1mg 98.27% ¥ 1462.50 ¥ 1462.50 2-3天
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¥ 0.00
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中文别名 来曲珠利(103337-74-2); 左沙丁胺;
英文别名 Letrazuril(103337-74-2);LETRAZURIL;Letrazurilo; Letrazurilum; AC1L1RUW; AC1Q4NLM;
CAS号 103337-74-2
SMILES O=C(N1)N(N=CC1=O)C2=CC(Cl)=C(C(C3=CC=C(F)C=C3)C#N)C(Cl)=C2
Inchi InChI=1S/C17H9Cl2FN4O2/c18-13-5-11(24-17(26)23-15(25)8-22-24)6-14(19)16(13)12(7-21)9-1-3-10(20)4-2-9/h1-6,8,12H,(H,23,25,26)
InchiKey XQKYUBTUOHHNDV-UHFFFAOYSA-N
分子式 Formula C17H9Cl2FN4O2
分子量 Molecular Weight 391.18
闪点 FP No data available
熔点 Melting point No data available
沸点 Boiling point No data available
Polarizability极化度 38.1±0.5 10-24cm3
密度 Density 1.5±0.1 g/cm3
蒸汽压 Vapor Pressure No data available
溶解度Solubility 生物体外In Vitro:DMSO溶解度≥ 165 mg/mL(421.80 mM)*"≥" means soluble可溶, but saturation unknown溶解度未知.
性状 固体粉末,Power
储藏条件 Storage conditions -20°C 3 years年 4°C 2 years年 / In solvent溶液中:-80°C 6 months月 -20°C 1 month月

来曲珠利(103337-74-2,Letrazuril)实验注意事项:
1.实验前需戴好防护眼镜,穿戴防护服和口罩,佩戴手套,避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生,必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储,并交于专业生物废气物处理公司处理,以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

Tags:来曲珠利试剂,来曲珠利杂质,来曲珠利中间体,来曲珠利密度,来曲珠利结构式,来曲珠利溶解度,来曲珠利合成,来曲珠利闪点,来曲珠利购买,来曲珠利MSDS,
产品说明 来曲珠利(103337-74-2,Letrazuril)是一种有效的抗HIV的有机化合物
Introduction(来曲珠利,103337-74-2)Letrazuril is anantiIVagent.
Application1来曲珠利(103337-74-2,Letrazuril)是一种抗艾滋病毒的化合物。Letrazuril已用于研究治疗HIV感染和隐孢子虫病的试验中。
Application2
Application3

来曲珠利(103337-74-2,Letrazuril)药理学:

来曲珠利(103337-74-2,Letrazuril)是一种抗艾滋病毒的化合物。Letrazuril已用于研究治疗HIV感染和隐孢子虫病的试验中。
A Study of Letrazuril in the Treatment of AIDS-Related Diarrhea Phase 1 Completed 2005-06-24
Hamour AA, et al. Successful treatment of AIDS-related cryptosporidial sclerosing cholangitis. AIDS. 1993 Nov;7(11):1449-51.
Letrazuril shows potential in AIDS-related cryptosporidiosis Inpharma Weekly 1994
Oral nitazoxanide and paromomycin inhalation for systemic cryptosporidiosis in a patient with AIDS Infection 1999
Chemotherapy of human and animal coccidioses: state and perspectives Parasitology Research 1996

来曲珠利(103337-74-2,Letrazuril)参考文献:


1、Treatment with letrazuril of refractory cryptosporidial diarrhea complicating AIDS M Loeb 1, C Walach, J Phillips, I Fong, I Salit, A Rachlis, S Walmsley

Abstract:Thirty-five AIDS patients (mean CD4 count 44 x 10(6)/L) with chronic cryptosporidiosis were treated with letrazuril at an initial oral daily dose of 50 mg in an open-label Phase I prospective trial. Treatment was continued for > or = 10 days and for as long as there was a response. The majority of subjects (91%), had previously failed paromomycin treatment. At baseline, 74% of patients had moderate (five to nine bowel movements per day) to severe (> 10 bowel movements per day) diarrhea. Twenty-three subjects (66%) had a clinical response within a mean of 1.7 weeks of treatment initiation. Twenty-two patients had a partial response (> 50% reduction in bowel movements per day for > or = 1 week), one patient had a complete response (two or fewer bowel movements per day). Of the responders, 15 (65%) had a clinical relapse with worsening diarrhea at an average of 1.2 months following initiation of letrazuril. The other eight (35%) had had symptom control for an average of 2.9 months from initiation of letrazuril to the latest follow-up. Microbiologic eradication was demonstrated in 10 (40%) of 25 patients with follow-up stool examinations. Seven patients (20%) experienced a rash, all within 1 week of starting the drug, and resolved in all patients when the drug was discontinued. In conclusion, severely immunocompromised AIDS patients with refractory cryptosporidiosis may show a modest, short-lived response to letrazuril. Microbiologic response is variable and relapse high. Rash is a major limiting side effect of the drug.


2、Pilot studies of azithromycin, letrazuril and paromomycin in the treatment of cryptosporidiosis   C Blanshard 1, D C Shanson, B G Gazzard

Abstract:Pilot studies of the safety and efficacy of 3 drugs thought to have anticryptosporidial activity were carried out to determine whether any of them are suitable for large-scale clinical trials. Open studies of the use of azithromycin, letrazuril and paromomycin in patients with acquired immunodeficiency syndrome (AIDS) and confirmed cryptosporidial diarrhoea for at least a month. Azithromycin 500 mg daily was ineffective. Letrazuril 150-200 mg daily was associated with an improvement in symptoms in 40% of patients treated and cessation of excretion of cryptosporidial oocysts in the stool in 70%; however biopsies remained positive. Paromomycin therapy was associated with a complete resolution of diarrhoea in 60% of patients treated and some improvement in symptoms in a further 5% but it did not eliminate the infection. None of the drugs had any major toxicities. Dose escalation studies of azithromycin should be performed. Letrazuril should be further investigated for efficacy in double-blind placebo-controlled trials. Paromomycin appears to result in prolonged symptomatic remission of cryptosporidial diarrhoea, but has no effect on cryptosporidial cholangitis.


 
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