Lumefantrine (Benflumetol)
(Synonyms: 苯芴醇; Benflumetol) 目录号 : GC32152
An antimalarial drug
Cas No.:82186-77-4
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
Lumefantrine is an antimalarial drug that is used in combination with artemether .1 The pairing of lumefantrine and artemether is a major form of oral artemisinin combination therapy used against uncomplicated P. falciparum malaria.2,3 Lumefantrine also blocks the rapidly activating delayed-rectifier potassium channel (IKr; IC50 = 8.1 ?M).4
1.Pascual, A., Parola, P., Benoit-Vical, F., et al.Ex vivo activity of the ACT new components pyronaridine and piperaquine in comparison with conventional ACT drugs against isolates of Plasmodium falciparumMalar. J.11(2012) 2.Askling, H.H., Bruneel, F., Burchard, G., et al.Management of imported malaria in EuropeMalar. J.11(2012) 3.Mayxay, M., Khanthavong, M., Chanthongthip, O., et al.Efficacy of artemether-lumefantrine, the nationally-recommended artemisinin combination for the treatment of uncomplicated falciparum malaria, in southern LaosMalar. J.11184(2012) 4.Du, L.P., Tsai, K.C., Li, M.Y., et al.The pharmacophore hypotheses of IKr potassium channel blockers: Novel class III antiarrhythmic agentsBioorg. Med. Chem. Lett.14(18)4771-4777(2004)
| Cas No. | 82186-77-4 | SDF | |
| 别名 | 苯芴醇; Benflumetol | ||
| Canonical SMILES | OC(CN(CCCC)CCCC)C1=CC(Cl)=CC(/C2=C\C3=CC=C(Cl)C=C3)=C1C4=C2C=C(Cl)C=C4 | ||
| 分子式 | C30H32Cl3NO | 分子量 | 528.94 |
| 溶解度 | DMSO : 2 mg/mL (3.78 mM);Water : < 0.1 mg/mL (insoluble) | 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 | 1.8906 mL | 9.4529 mL | 18.9057 mL |
| 5 mM | 0.3781 mL | 1.8906 mL | 3.7811 mL |
| 10 mM | 0.1891 mL | 0.9453 mL | 1.8906 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。
Pharmacodynamic interaction between Lumefantrine and desbutyl-benflumetol in Plasmodium falciparum in vitro
Wien Klin Wochenschr 2010 Oct;122 Suppl 3:61-5.PMID:20924691DOI:10.1007/s00508-010-1459-1.
The pharmacodynamic interaction between Lumefantrine and monodesbutyl-benflumetol has been investigated in 44 fresh isolates of patients with a Plasmodium falciparum infection from the region of Mae Sot (Thailand). Both substances proved to be effective against parasite maturation within the test concentration range, with monodesbutyl-benflumetol being effective at a lower concentration than Lumefantrine. Synergism between the two substances was evaluated with a combination of Lumefantrine and monodesbutyl-benflumetol at a ratio of 4.25:1. The geometric mean values for complete inhibition of schizont maturation were 1035.7 nM for Lumefantrine, 655 nM for monodesbutyl-benflumetol and 222.5 nM for the combination of both. An analysis for interaction according to the method of Berenbaum indicates a moderate synergism at the IC(50), which gets stronger with increasing ICs and reaches the highest level at the IC(99). The geometric mean of the sums of the FIC(50) is 0.73, of the FIC(90) it is 0.37 and of the FIC(99) it is 0.25.
Specific pharmacokinetic interaction between Lumefantrine and monodesbutyl-benflumetol in Plasmodium falciparum
Wien Klin Wochenschr 2007;119(19-20 Suppl 3):60-6.PMID:17987360DOI:10.1007/s00508-007-0861-9.
The blood schizontocidal activity of Lumefantrine, monodesbutyl-benflumetol (DBB) and a 999:1 combination of both compounds has been investigated in 26 fresh isolates of Plasmodium falciparum from northwestern Thailand, using the WHO standard protocol Mark II for determining the inhibition of schizont maturation. The geometric mean cut-off concentrations of schizont maturation (GMCOC) were 943.2 nM for Lumefantrine, 146.3 nM for DBB and 182.2 nM for the 999:1 combination of Lumefantrine and DBB. The EC(50) values were 27.3 nM for Lumefantrine, 5.7 nM for DBB, and 16.5 nM for the combination, and the EC(90) values 163.1 nM for Lumefantrine, 44.1 nM for DBB, and 78.3 nM for the combination. Despite the very low concentration in the combination, DBB exerted significant synergistic activity with Lumefantrine that was strongest at the EC(90) and EC(99) levels. Correlation analysis indicates that DBB is the leading determinant for the activity of the combination.
In vitro activity of Lumefantrine (Benflumetol) against clinical isolates of Plasmodium falciparum in Yaoundé, Cameroon
Antimicrob Agents Chemother 1998 Sep;42(9):2347-51.PMID:9736561DOI:10.1128/AAC.42.9.2347.
The in vitro antimalarial activity of the new Chinese synthetic drug, lumefantrine, also known as benflumetol (a fluorene derivative belonging to the aminoalcohol class), was determined by an isotopic microtest against 61 fresh clinical isolates of Plasmodium falciparum and compared with that of other established antimalarial agents. The geometric mean 50% inhibitory concentration of lumefantrine was 11.9 nmol/liter (95% confidence intervals, 10.4 to 13.6 nmol/liter; range, 3.3 to 25.6 nmol/liter). The in vitro activities of lumefantrine against the chloroquine-sensitive and the chloroquine-resistant isolates did not differ (P > 0.05). There was a significant positive correlation of responses between lumefantrine and two other aminoalcohols studied, mefloquine (r = 0.688) and halofantrine (r = 0.677), and between lumefantrine and artesunate (r = 0.420), suggesting a potential for in vitro cross-resistance. Our data suggest high in vitro activity of lumefantrine, comparable to that of mefloquine, and are in agreement with the promising results of preliminary clinical trials.
Interaction between Lumefantrine and monodesbutyl-benflumetol in Plasmodium falciparum in vitro
Wien Klin Wochenschr 2008;120(19-20 Suppl 4):85-9.PMID:19066780DOI:10.1007/s00508-008-1080-8.
The pharmacodynamic interaction between Lumefantrine and its monodesbutyl analogue (DBB) has been investigated in 35 fresh isolates of Plasmodium falciparum. Both compounds showed highly significant activity correlation. The geometric mean values for complete inhibition of schizont maturation (GMCOC) were 536,8 nM for Lumefantrine, 246.0 nM for DBB, 235,5 nM for LUM-DBB 999:1, and 155,2 nM for LUM-DBB 995:5, with significant activity differences between Lumefantrine and DBB as well as the LUM-DBB combinations. For the combination of Lumefantrine and DBB 995:5 the sums of the fractional inhibitory concentrations according to Berenbaum (SFIC) indicated marked synergism, the intensity of interaction rising with the effective inhibitory concentrations.
Comparative study on the in vitro activity of Lumefantrine and desbutyl-benflumetol in fresh isolates of Plasmodium vivax from Thailand
Wien Klin Wochenschr 2004;116 Suppl 4:47-52.PMID:15683043doi
The occurrence of chloroquine resistance in Plasmodium vivax underlines the need for monitoring the drug response of this important malaria parasite and for the evaluation of alternative therapeutic agents. In-vitro methods facilitate these tasks. This investigation employed a recently developed in-vitro micro-technique and validated it for Lumefantrine and desbutyl-benflumetol, a compound that was initially considered a metabolite of Lumefantrine. The studies were conducted in 2001 at Mae Sot, a town situated in northwestern Thailand near the border to Myanmar. Parallel in-vitro tests with Lumefantrine and desbutyl-benflumetol were carried out with 53 fresh isolates of P. vivax. For both compounds, the parasite showed a homogenous, log-normal inhibition pattern with nearly parallel log-probit regressions. The geometric mean drug concentrations effecting complete growth inhibition were 2361 nM for Lumefantrine and 187 nM for desbutyl-benflumetol. With p=3.264 x 10(-18) the difference was highly significant. The EC50 and EC90 values for Lumefantrine, 17.6 nM and 448.5 nM, respectively, were much higher as compared to those determined for desbutyl-benflumetol, with 1.5 nM and 39.7 nM. This difference expressed itself in a highly significant Power Ratio (PR) of 11.0. The activity of desbutyl-benflumetol in P. vivax exceeds that of Lumefantrine by one order of magnitude, suggesting a high, hitherto unexploited therapeutic potential of desbutyl-benflumetol.