- Naphthoquine phosphate
- Mefloquine hydrochloride
- Artemether (SM-224)
| DDD107498A novelmultiple-stage antimalarial agent |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
Related Biological Data
| Antimalarial experiment [1]: | |
Malaria parasites | Various malaria parasites |
Preparation method | This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
Reacting condition | 0.0001 ~ 10 μM |
Applications | DDD107498 showed excellent inhibition against 3D7 parasites, with the EC50 value of 1.0 nM. It also exhibited similar inhibition against several drug-resistant strains. Besides, DDD107498 was more potent than artesunate against a range of clinical isolates of both P. falciparum and P. vivax with the EC50 values of 0.81 nM and 0.51 nM respectively. In addition, the compound was non-toxic to human MRC5 and Hep-G2 cells at much higher concentrations. |
| Animal experiment [1]: | |
Animal models | NOD-scid IL-2R_null mice engrafted with human erythrocytes and infected with P. falciparum strain 3D70087/N9 |
Dosage form | 0.1, 0.3, 0.6, 1 or 3 mg/kg/day; p.o.; for 4 days |
Applications | In NOD-scid IL-2R_null mice engrafted with human erythrocytes and infected with P. falciparum strain 3D70087/N9, which were orally dosed daily for 4 days, the ED90 value on day 7 after infection was 0.95 mg/kg/day. Blood sampling from the infected SCID mice suggested the minimum parasiticidal concentration for DDD107498 was 10 ~ 13 ng/mL for asexual blood-stage infections. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Baragaa B, Hallyburton I, Lee MC et al. A novel multiple-stage antimalarial agent that inhibits protein synthesis. Nature. 2015 Jun 18;522(7556):315-20. | |
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| Cas No. | N/A | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 6-fluoro-2-(4-(morpholinomethyl)phenyl)-N-(2-(pyrrolidin-1-yl)ethyl)quinoline-4-carboxamide | ||
| Canonical SMILES | O=C(NCCN1CCCC1)C2=CC(C3=CC=C(CN4CCOCC4)C=C3)=NC5=CC=C(F)C=C52 | ||
| Formula | C27H31FN4O2 | M.Wt | 462.56 |
| Solubility | ≥14.05mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
DDD107498 is a potent and novel multiple-stage antimalarial agent against multiple life-cycle stages of the Plasmodium parasite. [1]DDD107498 has an acceptable safety profile and good pharmacokinetic properties. Translation elongation factor 2 (eEF2) has been identified as the molecular target of DDD107498. The factor eEF2 is responsible for the GTP-dependent translocation of the ribosome along messenger RNA, and is essential for protein synthesis. [1]DDD107498 showed excellent activity against Plasmodium falciparum 3D7 parasites with EC50 value of 1.0 nM, EC90 value of 2.4 nM and EC99 value of 5.9 nM. Furthermore, DDD107498 was more potent than artesunate in ex vivo assays against a range of clinical isolates of both P. falciparum (median EC50 = 0.81 nM (range 0.29–3.29 nM), n = 44) and P. vivax (median EC50 = 0.51 nM (range 0.25–1.39 nM), n = 28) collected from patients with malaria from southern Papua. [1]DDD107498 showed an EC50 < 1 nM against the liver schizont forms of P. berghei and Plasmodium yoelii. DDD107498 potently inhibited both male and female gamete formation from the gametocyte stage at similar concentrations [1.8 nM (95% CI 1.6–2.1 nM) and 1.2 nM (95% CI 0.8–1.6 nM)] respectively. DDD107498 blocked subsequent oocyst development in the mosquito after 7 days with an EC50 of 1.8 nM. [1]DDD107498 had a 90% reduction in parasitaemia (ED90) of 0.57 mg/kg after a single oral dose in mice infected with the rodent parasite Plasmodium berghei. When orally dosed daily for 4 days, the ED90 on day 7 after infection was 0.95 mg/kg/day. Blood sampling from the infected SCID (severe combined immunodeficiency) mice suggested a minimum parasiticidal concentration for DDD107498 of 10–13 ng/ml for asexual blood-stage infections. [1]In contrast, the compound was not toxic to human cells (MRC5 and Hep-G2 cells) at much higher concentrations (>20,000-fold selectivity). DDD107498 displayed excellent pharmacokinetic properties in preclinical species, including good oral bioavailability and long plasma half-life. DDD107498 showed good drug-like properties including metabolic stability when incubated with hepatic microsomes or hepatocytes from several species; good solubility in a range of different media; and low protein binding. [1]Reference:1.Baragaña B, Hallyburton I, Lee MC et al. A novel multiple-stage antimalarial agent that inhibits protein synthesis. Nature. 2015 Jun 18;522(7556):315-20.
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用DDBJ---350型便携式电导率仪测试，DJS-1C型铂黑电极，测的结果总是达不到要求，与纯水器上所显示的便高很多。
请问是测的方法不对或是所用的仪器不对？
你们所用的分析用水是怎么检测的？
多谢了！
急呀！
一、净水机：
1、功能：能够过滤掉自来水氯、杂质等，最后出来的水能够达到生饮的标准，保留了自来水中的对人体有用的矿物质；
2、特点：没有电机，不需要电源，靠水压驱动过滤。没有储水罐，比较好的为五级过滤，第一级为滤芯，第二和第三级为活性炭，第四级为中空丝膜或陶瓷过滤，第五级为精致活性炭，主要用于改善口感。
二、纯水机：
功能：过虑掉自来水中所有物质，出来的水是纯净水，相当于我们买的纯净水，跟净水机相比，净水机只能过虑到杂质之类，纯水机还把水中的各种矿物质都过虑掉了，比如水里面对人体有害的各种重金属，净水机出来的水虽然有矿物质，但是只是自来水含有的，很多矿物质是自来水无法提供的，也无法过滤掉各种矿物质，如果希望纯水机出来的水含有矿物质，可以单加一个麦饭石，这样出来的就是矿物质比较丰富的矿泉水了，当然，这样的矿泉水肯定比净水机出来的可以生饮的水好。
纯水机的选取首先要看您是做什么用途？不同型号和配置的水机，在各个指标的纯化程度是有倾斜的，这也决定了各型号的水机采取什么核心组件，进而决定价格。例如，如果做的实验室细胞培养类型的，那么就要求有机物、无极离子都要净，价格相对较高；如果是无机分析实验，那么对水中的无机离子去除要求较高，有机物物质相对不那么严格，价格会略低。
同时还取决于设备的产量等因素。
进口的密理博、pall，价格都在5万以上，甚至十多万；国产的比较杂，近万到数万元不等。
国产中锐思捷技术比较好，价格在3-5万之间，其他的如和泰或者乐枫。
1、机器本身故障
如果纯水机本身质量不好，对净水效果和出水量有直接影响，使用劣质纯水机水质没保障。问题一大堆。
解决办法：前期选购方面需要慎重。可以参考《纯水机选购注意事项》
2、水管漏水或堵塞
水管是运输水的唯一渠道，如果水管发生堵塞或漏水现象，对纯水机的出水量有直接影响。
解决办法：将水管漏水或者堵塞的地方剪切掉，如果堵塞或漏水范围太大，只能更换一条新的水管。
3、纯水机内部零件损坏
纯水机通过内部零件共同运作来净水，如果内部零件损坏，短期内虽然不会影响到产品的使用，但是会发生出水量降低的现象。长期不维修会引起产水二次污染。
解决办法：纯水机内部配件很多都是塑料组装，如果损坏了直接购买新的配置组装上去即可。不过要注意，在维修的时候要关闭进水球阀。
4、RO膜、反渗透膜杂质堆积
RO膜，反渗透膜是纯水机的灵魂，它们和出水量，净水效果等有直接关联，同时这种膜也是最容易发生问题的。纯水机出水少或者水质效果不好了很可能就是RO膜堆积杂质多了的原因。
解决办法：机器在使用一段时间之后（大概3-4个月）就对RO膜、反渗透膜进行清洗，确保水质中的污染物不会长时间堆积，这样是提升机器出水量，提升水质的最好办法。
菜鸟求救，大虾帮忙看看，感激不尽。
纯水机，是利用反渗透膜产出纯净水的净水机，属于直饮机。
二者区别：直饮机是一个统称，包含纯水机、超滤直饮机等；纯水机就是生产纯净水的机器，出水可以直接饮用。
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