Sulfalene (Sulfametopyrazine)
(Synonyms: 磺胺林; Sulfametopyrazine; AS-18908) 目录号 : GC32351
Sulfalene (SMPZ, Butadiene sulfone, 3-Sulfolene) is a cyclic organic chemical used as a versatile synthetic intermediate.
Cas No.:152-47-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Sulfalene (SMPZ, Butadiene sulfone, 3-Sulfolene) is a cyclic organic chemical used as a versatile synthetic intermediate.
| Cas No. | 152-47-6 | SDF | |
| 别名 | 磺胺林; Sulfametopyrazine; AS-18908 | ||
| Canonical SMILES | O=S(C1=CC=C(N)C=C1)(NC2=NC=CN=C2OC)=O | ||
| 分子式 | C11H12N4O3S | 分子量 | 280.3 |
| 溶解度 | DMSO : 100 mg/mL (356.76 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5676 mL | 17.838 mL | 35.6761 mL |
| 5 mM | 0.7135 mL | 3.5676 mL | 7.1352 mL |
| 10 mM | 0.3568 mL | 1.7838 mL | 3.5676 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
The influence of acetylator phenotype on the response to Sulfalene in individuals with chloroquine-resistant falciparum malaria
Am J Trop Med Hyg 1978 Mar;27(2 Pt 1):226-31.PMID:347958DOI:10.4269/ajtmh.1978.27.226.
The disposition of Sulfalene was studied in eight individuals before and during an infection with a chloroquine-resistant strain of Plasmodium falciparum. Isoniazid acetylator phenotype was determined in each individual prior to the administration of Sulfalene. Following the administration of Sulfalene before infection with malaria, a significant difference in half-life of non-acetylated Sulfalene and percent acetylation of Sulfalene in plasma was observed between rapid and slow acetylators. When Sulfalene was administered during malaria, this difference was no longer apparent. Individuals who did not respond to the therapeutic administration of Sulfalene alone were treated with a combination of Sulfalene and pyrimethamine. Three individuals were cured by Sulfalene without pyrimethamine and one was cured by the drug combination. Three of the four individuals who were not cured by any dose of Sulfalene or the drug combination were slow acetylators. There was no distinct correlation between clinical response and maximum levels or half-life of nonacetylated Sulfalene. These findings suggest that acetylator phenotype does not influence the therapeutic response of individuals infected with falciparum malaria to Sulfalene or to the combination of Sulfalene and pyrimethamine. Further information is presented, however, to confirm the importance of an as yet unidentified host factor(s) in determining therapeutic response to these agents.
Efficacy of artesunate with Sulfalene plus pyrimethamine versus praziquantel for treatment of Schistosoma mansoni in Kenyan children: an open-label randomised controlled trial
Lancet Infect Dis 2010 Sep;10(9):603-11.PMID:20705516DOI:10.1016/S1473-3099(10)70161-4.
Background: Schistosomiasis is an important parasitic disease in Kenya. Decreasing susceptibility of schistosomes to praziquantel, the major drug used to reduce disease morbidity, has made assessment of new antischistosomal drugs a priority. We aimed to assess the safety and efficacy of an artesunate-based combination drug in the treatment of schistosomiasis. Methods: In this open-label randomised trial in Rarieda district of western Kenya, we enrolled school children (aged 6-15 years) who had Schistosoma mansoni infection according to duplicate Kato-Katz thick smears from a stool sample. Computer-generated block randomisation was used to assign children (1:1) to receive artesunate (100 mg) with Sulfalene (also known as sulfamethoxypyrazine; 250 mg) plus pyrimethamine (12.5 mg) as one dose every 24 h for 3 days or one dose of praziquantel (40 mg/kg per day). The primary efficacy endpoint was the number of participants cured 28 days after treatment. Analysis was by intention to treat. This trial is registered with ClinicalTrials.gov, number NCT01054651. Results: Between October and December, 2009, 212 children were enrolled and assigned to receive artesunate with Sulfalene plus pyrimethamine (n=106) or praziquantel (n=106). 69 patients (65%) were cured in the praziquantel treatment group compared with 15 (14%) in the artesunate with Sulfalene plus pyrimethamine treatment group (p<0.0001). Adverse events were less common in patients taking artesunate with Sulfalene plus pyrimethamine than in those taking praziquantel (22% [n=23] vs 49% [n=52], p<0.0001), and no drug-related serious adverse events occurred. Interpretation: The standard treatment with praziquantel is more effective than artesunate with Sulfalene plus pyrimethamine in the treatment of children with S mansoni infection in western Kenya. Whether artemisinin-based combination therapy has a role in the treatment of schistosomiasis is unclear.
Host failure in treatment of malaria with Sulfalene and pyrimethamine
Ann Intern Med 1975 Feb;82(2):219-23.PMID:1090224DOI:10.7326/0003-4819-82-2-219.
An individual infected with a multidrug-resistant strain of Plasmodium falciparum failed to respond to treatment with Sulfalene and pyrimethamine. Subinoculation studies showed that parasite resistance to the drug combination was not present. Plasma levels of Sulfalene and pyrimethamine in this individual were similar to those of three individuals, subinoculated from him, who were cured by the drug combination. Erythrocyte levels of Sulfalene in this individual were similar to those in an individual, subinoculated from him, who was cured by the drug combination. After treatment with the drug combination, in vitro tests showed similar antimalarial activity in the serum of this individual in comparison with the serum of this individual in comparison with the serum of an individual subinoculated from him. The failure of this individual to respond to treatment with Sulfalene and pyrimethamine is attributed to an undefined host factor (or factors) that appear(s) to be present in his erythrocytes.
Sulfametopyrazine prophylaxis in chronic bronchitis
Br J Dis Chest 1978 Jul;72(3):231-4.PMID:359024DOI:10.1016/0007-0971(78)90047-5.
From a double-blind randomized controlled trial by 32 general practitioners on 218 patients with chronic bronchitis it appeared that Sulfametopyrazine given once a week over one winter reduced the number of respiratory illnesses and the loss of time from work to about half that of a control group. It had no effect on time off work in individual spells of illness nor on the amount and purulence of sputum. Side-effects were few and mild.
Sulfalene concentrations in plasma and blood cells of Plasmodium falciparum malaria cases after treatment with metakelfin using high-performance liquid chromatography
J Chromatogr B Biomed Sci Appl 1998 Sep 4;714(2):390-4.PMID:9766882DOI:10.1016/s0378-4347(98)00222-9.
A reversed-phase high-performance liquid chromatographic method using acetonitrile-methanol-1 M perchloric acid-water (25:9:0.8:95, v/v/v) at a flow-rate of 1.0 ml min(-1) on LiChrospher 100 RP 18 column (250 x 4 mm; 5 microm) with UV (254 nm) detection has been developed for the determination of Sulfalene in plasma and blood cells after oral administration of the antimalarial drug metakelfin. Calibration curves were linear in the range 0.5-100 microg ml(-1). The limit of quantification was 50 ng ml(-1). Within-day and day-to-day coefficients of variation averaged 3.84 and 5.31%, respectively. Mean extraction recoveries of Sulfalene from plasma and blood cells were 87.21 and 84.65%, respectively. Mean concentrations of Sulfalene in plasma of P. falciparum cases on days 2, 7 and 15 were 44.58, 14.90 and 1.70 microg ml(-1), respectively; in blood cells concentrations of Sulfalene were 7.77, 3.25 and 0.75 microg ml(-1), respectively, after oral treatment with two tablets (1000 mg) of metakelfin. Significant difference was recorded on day 2 for Sulfalene concentration in blood cells of healthy and P. falciparum cases (t=9.49; P<0.001).