China Largest Manufacturer factory sales Lumefantrine CAS 82186-77-4 CAS NO.82186-77-4

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Lumefantrine Basic information Antimalarial drug Physical and Chemical Properties Pharmacokinetics Dosage Adverse reactions Precautions Product Name: Lumefantrine Synonyms: (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 CAS: 82186-77-4 MF: C30H32Cl3NO MW: 528.94 EINECS: 617-303-4 Product Categories: Pharmaceutical intermediates;Antibiotics;Amines;Aromatics;Intermediates & Fine Chemicals;API;Pharmaceuticals Mol File: 82186-77-4.mol   Lumefantrine Chemical Properties 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)   Safety Information WGK Germany  3 HS Code  29221950 Hazardous Substances Data 82186-77-4(Hazardous Substances Data) MSDS Information   Lumefantrine Usage And Synthesis 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 (Item No. 11815). 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 (IKr; IC50 = 8.1 μM). Chemical Properties Yellow Solid Uses Inhibits hemozoin formation. Antimalarial 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

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Leader Biochemical Group is a large leader incorporated industry manufacturers and suppliers of advanced refined raw materials From the year of 1996 when our factory was put into production to year of 2020, our group has successively invested in more than 52 factories with shares and subordinates.We focus on manufacture Pharm & chemicals, functional active ingredients, nutritional Ingredients, health care products, cosmetics, pharmaceutical and refined feed, oil, natural plant ingredients industries to provide top quality of GMP standards products.All the invested factories' product lines cover API and intermediates, vitamins, amino acids, plant extracts, daily chemical products, cosmetics raw materials, nutrition and health care products, food additives, feed additives, essential oil products, fine chemical products and agricultural chemical raw materials And flavors and fragrances. Especially in the field of vitamins, amino acids, pharmaceutical raw materials and cosmetic raw materials, we have more than 20 years of production and sales experience. All products meet the requirements of high international export standards and have been recognized by customers all over the world. Our manufacture basement & R&D center located in National Aerospace Economic & Technical Development Zone Xi`an Shaanxi China. Now not only relying on self-cultivation and development as well as maintains good cooperative relations with many famous research institutes and universities in China. Now, we have closely cooperation with Shanghai Institute of Organic Chemistry of Chinese Academy of Science, Beijing Institute of Material Medical of Chinese Academy of Medical Science, China Pharmaceutical University, Zhejiang University. Closely cooperation with them not only integrating Science and technology resources, but also increasing the R&D speed and improving our R&D power. Offering Powerful Tech supporting Platform for group development. Keep serve the manufacture and the market as the R&D central task, focus on the technical research.  Now there are 3 technology R & D platforms including biological extract, microorganism fermentation and chemical synthesis, and can independently research and develop kinds of difficult APIs and pharmaceutical intermediates. With the strong support of China State Institute of Pharmaceutical Industry (hereinafter short for CSIPI), earlier known as Shanghai Institute of Pharmaceutical Industry (SIPI), we have unique advantages in the R & D and industrialization of high-grade, precision and advanced products.  Now our Group technical force is abundant, existing staff more that 1000 people, senior professional and technical staff accounted for more than 50% of the total number of employees, including 15 PhD research and development personnel, 5 master′ S degree in technical and management personnel 9 people. We have advanced equipment like fermentation equipment and technology also extraction, isolation, purification, synthesis with rich production experience and strict quality control system, According to the GMP required, quickly transforming the R&D results to industrial production in time, it is our advantages and our products are exported to North and South America, Europe, Middle East, Africa, and other five continents and scale the forefront in the nation, won good international reputation.  We believe only good quality can bring good cooperation, quality is our key spirit during our production, we are warmly welcome clients and partner from all over the world contact us for everlasting cooperation, Leader will be your strong, sincere and reliable partner in China.

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Lumefantrine Basic information Antimalarial drug Physical and Chemical Properties Pharmacokinetics Dosage Adverse reactions Precautions Product Name: Lumefantrine Synonyms: (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 CAS: 82186-77-4 MF: C30H32Cl3NO MW: 528.94 EINECS: 617-303-4 Product Categories: Pharmaceutical intermediates;Antibiotics;Amines;Aromatics;Intermediates & Fine Chemicals;API;Pharmaceuticals Mol File: 82186-77-4.mol   Lumefantrine Chemical Properties 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)   Safety Information WGK Germany  3 HS Code  29221950 Hazardous Substances Data 82186-77-4(Hazardous Substances Data) MSDS Information   Lumefantrine Usage And Synthesis 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 (Item No. 11815). 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 (IKr; IC50 = 8.1 μM). Chemical Properties Yellow Solid Uses Inhibits hemozoin formation. Antimalarial 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