Piperaquine
(Synonyms: 磷酸哌喹,Piperaquinoline) 目录号 : GC13875
An antimalarial agent
Cas No.:4085-31-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 9.8 to 217.3 nM for P. falciparum isolates
Piperaquine, an antimalarial drug, is first synthesised in the 1960s and extensively used as prophylaxis and treatment during the next 20 years.
In vitro: In 280 P. falciparum isolates, the IC50 for piperaquine ranged from 9.8 nM to 217.3 nM and a significant but low correlation was observed between the IC50 values for piperaquine and chloroquine. However, the coefficient of determination indicated that only 2.1% of the variation in the response to piperaquine was explained by the variation in the response to chloroquine. Moreover, the mean value for piperaquine was 74.0 nM in the Pfcrt K76 wild-type group and 87.7 nM in the 76T mutant group and such difference was not significant [1].
In vivo: Male SD rats were orally administered piperaquine or as a short-term i.v. infusion. Results showed that piperaquine disposition was best described by a 3-compartment model with a rapid initial distribution phase after i.v. administration. The PK of piperaquine was characterized by a low clearance, a large volume of distribution and a long terminal half-life [2].
Clinical trial: The safety and efficacy of a combination of dihydroartemisinin (DHA) and piperaquine was assessed in patients with uncomplicated falciparum malaria. Mean total DHA and piperaquine doses were 9.1 and 73.9 mg/kg, respectively, for children and 6.6 and 52.9 mg/kg for adults. Results showed that excluding the results for 1 child who died, there was a 96.9% 28-day cure rate. Side effects were reported by 22 patients but did not necessitate premature cessation of therapy [3].
References:
[1] Pascual A et al. In vitro piperaquine susceptibility is not associated with the Plasmodium falciparum chloroquine resistance transporter gene. Malar J. 2013 Nov 25;12:431.
[2] Tarning J, Lindegardh N, Sandberg S, Day NJ, White NJ, Ashton M. Pharmacokinetics and metabolism of the antimalarial piperaquine after intravenous and oral single doses to the rat. J Pharm Sci. 2008 Aug;97(8):3400-10.
[3] Denis MB, Davis TM, Hewitt S, Incardona S, Nimol K, Fandeur T, Poravuth Y, Lim C, Socheat D. Efficacy and safety of dihydroartemisinin-piperaquine (Artekin) in Cambodian children and adults with uncomplicated falciparum malaria. Clin Infect Dis. 2002 Dec 15;35(12):1469-76.
| Cas No. | 4085-31-8 | SDF | |
| 别名 | 磷酸哌喹,Piperaquinoline | ||
| 化学名 | 4,4'-(1,3-propanediyldi-4,1-piperazinediyl)bis[7-chloro-quinoline | ||
| Canonical SMILES | ClC1=CC2=C(C=C1)C(N3CCN(CC3)CCCN4CCN(CC4)C5=C6C=CC(Cl)=CC6=NC=C5)=CC=N2 | ||
| 分子式 | C29H32Cl2N6 | 分子量 | 535.5 |
| 溶解度 | ≤0.2mg/ml in DMSO | 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 | 1.8674 mL | 9.3371 mL | 18.6741 mL |
| 5 mM | 0.3735 mL | 1.8674 mL | 3.7348 mL |
| 10 mM | 0.1867 mL | 0.9337 mL | 1.8674 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。