- 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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有些同行用娃哈哈,能满足药典吗?纯水机呢?
我问弱了,请大家不要嘲笑我。
我想咨询的是ELIX的处理柱(好象叫PRO-GUARD),多长时间换一次,我们这里在用水不是很大量的情况下半年就不行了,总是提示低压报警,现在刚换了三个月,又开始报警了,是否我们这里水质极差还是机器有问题?
该怎么解决呢,一个柱子近3000大洋,太贵了,还不如直接买纯净水划的来
主要看你具体的需要,
适合你的才是最好的。
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。
纯水机的价格影响因素除了进口品牌和国产品牌的差异外,主要取决于产量、用途以及其他特殊要求。
综合来看,除非有硬性规定或者需要采用进口品牌来提升实验室形象,否则建议选择国产品牌即可,因为实际上纯水机作为实验室常规设备,在工艺技术上知名度较高的国产品牌已足与进口相媲美,且价格仅为进口的1/3左右。
你需要先确定采购水机的主要实验用途,不同的实验用途,对水的要求是不一样的,从而也决定了所采购纯水机的配置,进而决定价格。
水中需纯化的物质主要有:无机离子、总有机碳(TOC)、微小粒子、微生物(内毒素、热原)、弱电解质。根据对以上物质的去除度,生产出来的纯水分为三个级别:初级纯水、中级水、超纯水。一般来水,仅产初级产水的纯水机价格在1.2万左右(产量10L);同时产初级纯水和超纯水的纯水机价格在(2-3万左右,产量10L)。
此外,还需要确定具体的实验用途,不同的实验用水,对于水中的物质去除度是有区分的,会有一定的倾斜度,比如细胞培养型实验,就对无机离子和TOC去除度要求严格;无机分析实验的话对无机离子去除要求高。
国产中,锐思捷、力康都还不错。
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!
纯水机是属于科学仪器,用途在于实验室科研,工艺技术相较于净水器复杂很多,设备所用的组件和耗材也比净水器多,原则上可以说:净水器的超级升级版就是纯水机。
水中的杂质有微小颗粒、无机离子(钙离子、钠离子、镁离子等)、微生物(内毒素、热原)、弱电解质、有机物。
净水器是将水中的有害物质(污染物)净化成可直接饮用的水,但是水中仍有较多的无机离子和部分有机物,这对人体无害,甚至可被人体吸收利用;纯水机又分为初级纯水机和超纯水机,力求纯化后只剩下水,不含其它任何物质。
净水器的工艺是:预处理-反渗透;
纯水机的工艺是:预处理-反渗透-紫外消毒-DI离子交换-超滤(若需要);
净水器售价在几千元即可,最高不超过一万;纯水器可由近万元至十多万。