Lumefantrine
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Lumefantrine ??
- ???
- 129-131°C
- ?? ?
- 642.5±55.0 °C(Predicted)
- ??
- 1.252
- ?? ??
- 15-25°C
- ???
- DMSO: ≥20mg/mL
- ?? ?? (pKa)
- 13.44±0.20(Predicted)
- ??? ??
- ??
- ??
- ???
- Merck
- 14,5597
- ?? ??
- ???(???)
- InChIKey
- DYLGFOYVTXJFJP-MYYYXRDXSA-N
- SMILES
- C12C(C(CN(CCCC)CCCC)O)=CC(Cl)=CC=1/C(=C\C1C=CC(Cl)=CC=1)/C1C=C(Cl)C=CC2=1
- CAS ??????
- 82186-77-4(CAS DataBase Reference)
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- ?? ? ???? ?? (GHS)
| WGK ?? | 3 | ||
|---|---|---|---|
| HS ?? | 29221950 | ||
| ???? ??? | 11 - Combustible Solids | ||
| ?? ?? ??? | 82186-77-4(Hazardous Substances Data) |
| ????(GHS): |
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| ?? ?: | Warning | |||||||||||||||||||||||||||||||||||
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Lumefantrine C??? ??, ??, ??
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Yellow Solid?? ??
Lumefantrine has been used:to study its effect on ex-vivo Plasmodium falciparum sensitivity using the tritiated hypoxanthine-based assay
as a standard in the quantification of combined tablet formulation using HPTLC
as a drug molecule in in vitro growth inhibition assay for in vitro B. caballi growth inhibition studies
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ChEBI: Lumefantrine is an antimalarial drug used in combination with artemether for the treatment of multi-drug resistant strains of falciparum malaria.Antimicrobial activity
Lumefantrine has marked blood schizonticidal activity against a wide range of plasmodia, including chloroquineresistant P. falciparum. The 50% and 90% effective concentrations (EC50 and EC90) in vitro are similar: <10 and 40 nmol/L, respectively. The racemate and the two enantiomers exhibit similar activities. Blood schizonticidal activity of desbutylbenflumetol is four to five times greater than benflumetol in vitro.??
Treatment with artemether–lumefantrine can select for polymorphisms in the P. falciparum pfmdr1 gene. Resistance has been selected experimentally in murine malaria.?? ??
Lumefantrine was developed in China. Itsmechanism of action is poorly understood. There is some evidencethat it inhibits the formation of β-hematin by forming acomplex with hemin. Lumefantrine is very lipophilic and is marketed in combination with the lipophilic artemesininderivedartemether.Pharmaceutical Applications
A dichlorobenzylidene derivative given orally in combination with artemether.Pharmacokinetics
Bioavailability after oral administration is variable; absorption is substantially increased by co-administration with food, particularly with a high fat content. Peak plasma concentrations occur after 6–8 h. The elimination half-life is 4–6 days. It is almost completely protein bound and metabolized mainly in the liver by CYP3A4.Clinical Use
Treatment of P. falciparum infections (including mixed infections) in a fixed-dose combination treatment with artemether.???
The most common adverse effects in combination with artemether include headache, dizziness and gastrointestinal disturbances.?? ??
Primaquine is almost totally metabolized by CYP3A4 (99%), with the primary metabolite being carboxyprimaquine. Trace amounts of N-acetylprimaquine plus aromatic hydroxylation and conjugation metabolites also have been reported.Lumefantrine ?? ?? ? ???
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Lumefantrine ?? ??
???( 501)?? ??
| ??? | ?? | ??? | ?? | ?? ? | ?? |
|---|---|---|---|---|---|
| Vinsce Bio pharm (Suzhou) Co Ltd | +86-13962217456 |
info@vinsce.com | China | 38 | 58 |
| Hebei Chuanghai Biotechnology Co,.LTD | +86-86-13131129325 |
sales1@chuanghaibio.com | China | 5218 | 58 |
| Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 |
info@fdachem.com | China | 20111 | 58 |
| Shaanxi TNJONE Pharmaceutical Co., Ltd | |
sarah@tnjone.com | China | 1139 | 58 |
| Hefei Lbao Physical & Chemical Science Co.,Ltd | +1-5184799099; |
lbaochemicals@gmail.com | China | 670 | 58 |
| Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21531 | 55 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 |
ivan@atkchemical.com | China | 32998 | 60 |
| Hefei TNJ Chemical Industry Co.,Ltd. | +86-0551-65418679 +86-18949832763 |
info@tnjchem.com | China | 2984 | 55 |
| career henan chemical co | +86-0371-86658258 |
sales@coreychem.com | China | 29766 | 58 |
| Xiamen AmoyChem Co., Ltd | +86-86-5926051114 |
sales@amoychem.com | China | 6361 | 58 |