Lumefantrine

ChemicalBook > CAS DataBase List > Lumefantrine

Antimalarial drug Physical and Chemical Properties Pharmacokinetics Dosage Adverse reactions Precautions

Product Name: Lumefantrine
CAS No.: 82186-77-4
Chemical Name: Lumefantrine
Synonyms: LuMefentrine;benflumetol;Benwuchun;CPG-56695;Benflumelol;umefantrine;A + alcohol;Benflumentol;Lumefantrine;Lumefruntrine
CBNumber: CB7854882
Molecular Formula: C30H32Cl3NO
Formula Weight: 528.94
MOL File: 82186-77-4.mol

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Lumefantrine Property

Melting point:: 129-131°C
Boiling point:: 642.5±55.0 °C(Predicted)
Density: 1.252
storage temp.: 15-25°C
solubility: DMSO: ≥20mg/mL
pka: 13.44±0.20(Predicted)
form: powder
color: yellow
Merck: 14,5597
CAS DataBase Reference: 82186-77-4(CAS DataBase Reference)

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Safety

WGK Germany: 3
HS Code: 29221950
Hazardous Substances Data: 82186-77-4(Hazardous Substances Data)

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: L5420
Product name: Lumefantrine
Packaging: 5mg
Price: $118
Updated: 2024/03/01

Sigma-Aldrich

Product number: 1370746
Product name: Lumefantrine
Purity: United States Pharmacopeia (USP) Reference Standard
Packaging: 100mg
Price: $436
Updated: 2024/03/01

TCI Chemical

Product number: L0256
Product name: Lumefantrine
Purity: >98.0%(HPLC)(T)
Packaging: 5g
Price: $38
Updated: 2024/03/01

TCI Chemical

Product number: L0256
Product name: Lumefantrine
Purity: >98.0%(HPLC)(T)
Packaging: 25g
Price: $110
Updated: 2024/03/01

Cayman Chemical

Product number: 20678
Product name: Lumefantrine
Purity: ≥98%
Packaging: 1g
Price: $32
Updated: 2024/03/01

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Lumefantrine Chemical Properties,Usage,Production

Antimalarial drug

Benflumetol and artemether are the widely used antimalarial drugs currently in clinical , they are the main ingredients of the well-known anti-malarial drugs called Compound artemether of Novartis ,which can kill plasmodia asexual, insecticidal rate is high, the cure rate is about 95%, but it is invalid in the pre-erythrocytic stage and gametophyte . Animal experiments suggest it is drug with micro toxicity,but the mutagenic and teratogenic tests are negative. It is mainly used for the treatment of falciparum malaria in clinical, especially for the chloroquine-resistant falciparum malaria treatment.

Physical and Chemical Properties

Yellow crystalline powder, bitter almond smell, tasteless. Soluble in chloroform, slightly soluble in acetone, almost insoluble in alcohol, melting point of 125~131 ℃.

Pharmacokinetics

Oral absorption is slow, elimination is also slow,it can stay a long time in the body . Tmax after administration is 4~5h, t1/2 is 24~72h.

Dosage

4d therapy: Adults eat 800mg at draught on the first day ,on day 2, 3, 4, each 400mg at draught; children daily take 8mg/kg at draught, and continue for 4d, the first dose is doubled, but the first dose does not exceed the maximum dose of 0.6g.
The above information is edited by the chemicalbook of Tian Ye.

Adverse reactions

There are no significant adverse reactions, a small number of patients suffer with electrocardiographic Q~T interval transient mild extending.

Precautions

Patients with heart, kidney dysfunction,should use with caution. After symptoms are controlled in patients with malignant malaria and the parasite is killed in the pre-erythrocytic stage ,primaquine can be used to kill gametocytes. It is saved in the dark, sealed, cool and dry place.

Description

Lumefantrine is a derivative of halofantrine that has been reported to exhibit antimalarial activity when combined with artemether in the treatment of multidrug-resistant Plasmodium falciparium . No evidence of cardiotoxicity has been reported with this combination, which may offer promise for successful treatment of resistant organisms.

Description

Lumefantrine is an antimalarial drug that is used in combination with artemether . The pairing of lumefantrine and artemether is a major form of oral artemisinin combination therapy used against uncomplicated P. falciparum malaria. Lumefantrine also blocks the rapidly activating delayed-rectifier potassium channel (I_Kr; IC₅₀ = 8.1 μM).

Chemical Properties

Yellow Solid

Uses

A drug used in the treatment of malaria. Antimalarials are usually classified on the basis of their action against Plasmodia at different stages in their life cycle in the human.

Uses

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

Uses

Inhibits hemozoin formation. Antimalarial.

Definition

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.

Acquired resistance

Treatment with artemether–lumefantrine can select for polymorphisms in the P. falciparum pfmdr1 gene. Resistance has been selected experimentally in murine malaria.

General Description

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.

Biochem/physiol Actions

Lumefantrine is is an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.

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.

Side effects

The most common adverse effects in combination with artemether include headache, dizziness and gastrointestinal disturbances.

Metabolism

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 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Lumefantrine manufacturers

Henan Fengda Chemical Co., Ltd

Product: Lumefantrine 82186-77-4
Price: US $36.00-1.20/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: g-kg-tons, free sample is available
Release date: 2024-04-16

WUHAN FORTUNA CHEMICAL CO., LTD

Product: Lumefantrine 82186-77-4
Price: US $1.00/KG
Min. Order: 1KG
Purity: 98.0%~102.0% ,USP36
Supply Ability: 500kg/month
Release date: 2021-06-04

Hebei Mingeng Biotechnology Co., Ltd

Product: Benflumetol 82186-77-4
Price: US $300.00/KG
Min. Order: 10g
Purity: 99.8%
Supply Ability: 10 MT
Release date: 2021-11-11

82186-77-4, LumefantrineRelated Search:

Methylene Blue Dichlorodiphenylsilane Acetonitrile 4,4'-Diphenylmethane diisocyanate Sulfamic acid Diethylene glycol dibenzoate Basic Violet 1 Dichloroethane EC 2.6.1.2 Acetaminophen Methylparaben Dichloromethylphenylsilane 3,4'-DIAMINODIPHENYLMETHANE Methanol Methyl acrylate Methyl Polyol benzoate Methylene Chloride

(9Z)-2,7-Dichloro-9-[(4-chlorophenyl)methylene]-α-[(dibutylamino)methyl]-9H-fluorene-4-methanol

CPG-56695

Benwuchun

Benflumentol

benflumetol

Lumefantrine

BENFLUMETOL (OR LUMEFANTRINE)

(9Z)-2,7-Dichloro-9-[(4-chlorophenyl)methylene]-a-[(dibutylamino)methyl]-9H-fluorene-4-methanol

2-Dibutylamino-1-[2,7-dichloro-9-[1-(4-chlorophenyl)meth-(Z)-ylidene]-9H-fluoren-4-yl]ethanol

Benflumelol

dl-Benflumelol

(z)-2,7-dichloro-9-[(4-chlorophenyl)methylene]-alpha-[(dibutylamino)methyl]-9h-fluorene-4-methanol

Lumefruntrine

LUMEFRUNTRINE (BENFLUMETOL)

Lumefantrine (100 mg)

LuMefrantine-D9

(Z)-2-(DibutylaMino)-1-(2,7-dichloro-9-(4-chlorobenzylidene)-9H-fluoren-4-yl)ethanol

LuMefentrine

LuMenfantrine

LuMenfantrine-d9

BENFLUMETOLUM

Lumefantrine, 98%, Inhibits hemozoin formation. Antimalarial.

Lumefantrine [Benflumetol]

(+-)-2,7-Dichloro-9-((Z)-p-chlorobenzylidene)-alpha((dibutylamino)methyl)fluorene-4-methanol

Lumefantrine&gt

Lumefantrine Lumefantrine

umefantrine

9H-Fluorene-4-methanol, 2,7-dichloro-9-[(4-chlorophenyl)methylene]-α-[(dibutylamino)methyl]-, (9Z)-

(9Z)-2,7-Dichloro-9-[(4-chlorophenyl)methylene]-alpha-[(dibutylamino)methyl]-9H-fluoren-4-methanol

Lumefantrine USP/EP/BP

Lumefrantrine USP/EP/BP

Lumefantrine oxalate salt

Lumefantrine D9Q: What is Lumefantrine D9 Q: What is the CAS Number of Lumefantrine D9 Q: What is the storage condition of Lumefantrine D9 Q: What are the applications of Lumefantrine D9

LumefantrineQ: What is Lumefantrine Q: What is the CAS Number of Lumefantrine Q: What is the storage condition of Lumefantrine Q: What are the applications of Lumefantrine

Lumefantrine (1370746)

A + alcohol

2H9]-Lumefantrine oxalate salt

Lumefantrine, ≥ 98.0%

82186-77-4

C30H32Cl3NO

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82186-77-4