China Largest Manufacturer factory Supply Artesunate CAS 88495-63-0 CAS NO.88495-63-0

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Artesunate Basic information Antiparasitic drug Dosage and administration Clinical application Uses Product Name: Artesunate Synonyms: ARTENSUNATE;Butanedioic acid, 1-[(3R,5aS,6R,8aS,9R,10S,12R,12aR)-decahydro-3,6,9-trimethyl-3,12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin-10-yl] ester;Artesunate (3R,5aS,6R,8aS,9R,10S,12R,12aR)-Decahydro-3,6,9-trimethyl-3,12-epoxy-12H-pyrano(4,3-j)-1,2-benzodioxepin-10-ol hydrogen succinate;ARTESUNATE;ArtesunateC19H28O8;Artemisinin monosuccinate;Artesunic Acid;Butanedioic Acid Mono(3R,5aS,6R,8aS,9R,10R,12R,12aR)-decahydro-3,6,9-trimethyl-3,12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin-10-yl] Ester CAS: 88495-63-0 MF: C19H28O8 MW: 384.42 EINECS: 618-170-5 Product Categories: natural product;Antimalarial;Natural Plant Extract;plant extract;Herb extract;Inhibitors;Active Pharmaceutical Ingredients;Intermediates & Fine Chemicals;Pharmaceuticals;88495-63-0 Mol File: 88495-63-0.mol   Artesunate Chemical Properties Melting point  132-1350C Boiling point  431.1°C (rough estimate) density  1.2076 (rough estimate) refractive index  1.4430 (estimate) storage temp.  2-8°C solubility  acetone: soluble33.4mg/mL form  crystalline powder pka 4.28±0.17(Predicted) color  white to off-white Merck  14,818 Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.   Safety Information Hazard Codes  Xn Risk Statements  20/21/22 Safety Statements  24/25 WGK Germany  3 HS Code  29419090 Hazardous Substances Data 88495-63-0(Hazardous Substances Data) MSDS Information   Artesunate Usage And Synthesis Antiparasitic drug Artesunate is a kind of commonly used anti-parasitic drug and belongs to reduced artemisinin succinate monoester, and is the derivative of artemisinin containing a sesquiterpene lactone structure, and has a stronger efficacy on treating parasite than artemisinin and is also effective on treating chloroquine resistant strains. It acts on the Plasmodium schizonts on the erythrocytic stage. It takes effect by inhibiting cytochrome oxidase through reduced artemisinin to achievement of the inhibition on the function of cytochrome oxidase of malaria parasite surface membrane-food vacuole membrane, mitochondrial membrane, and thus blocking the supplying of nutrition from the host cell cytoplasm. It has a strong killing effect on the asexual form of plasmodium with a rapid efficacy enabling the rapid control of the onset of malaria. It has good efficacy on treating cerebral malaria, falciparum malaria and vivax malaria with similar efficacy in treating chloroquine-resistant strain of the falciparum malaria, especially with more significant effect on treating cerebral malaria. It can quickly control the emergence of malaria but has no effect on falciparum malaria gametophyte. It has a shorter T1/2 than artemether with blood concentration rapid decreasing after intravenous injection. Its T1/2 is about 30 min. It is widely distributed in the body with the content in intestine, liver, kidney being relative high. Urine and fecal excretion account for only a small fraction. It mainly undergoes metabolic conversion. It is clinically suitable for rescue of critically ill patients with acute malaria and can be used as the first-choice drug for the treatment of patients with cerebral malaria and a variety of dangerous malaria. But its shortcoming is the recrudescence rate. No adverse reactions have been observed at the recommended therapeutic dose; the application of large doses may cause a transient reduction of the outer peripheral reticulocyte which will return to normal level after stopping drug. Women within 2 months of pregnancy should be disabled. Whether it will cause teratogenicity demands further study. Dosage and administration Powder: 60mg; each artesunate is also attached with one 5% sodium bicarbonate injection. Upon application, first dissolve the drug in sodium bicarbonate injection, and then diluted to 10 ml with glucose injection after intravenous infusion at a rate of 3~4ml/min. For the treatment of patients of chloroquine-resistant falciparum malaria: 60 mg per time with the first dose being doubled; intravenously inject 1 times per day with 4 days as a course of treatment. The total dose is 300mg. When the symptom gets controlled, you can change with other anti-malarial drugs to reduce the recrudescence rate. The exact dosage and tablets should be according to the exact condition. The above information is edited by the Chemicalbook of Dai Xiongfeng. Clinical application The clinical application of artesunate has been as long as ten years. It is made through using the artemisia annua grass which is unique in China as raw material for extracting the active ingredient artemisinin and further going through chemical synthesis. Its major role is in treating plasmodia asexual form. It is also currently the only artemisinin derivatives which can be made into water-soluble formulation. It can be used to kill the parasite in inner phase of red blood cells to achieve the anti-malarial effect, and therefore being used in patients with various types of malaria, especially for treating and saving the patients with anti-chloroquine and anti-piperaquine falciparum malaria and severe-type cerebral malaria. It is characterized by high anti-malarial activity, high rate of fever abatement, short parasite clearance time and low drug toxic and side effects. It is the first-choice of drugs for the treatment of severe malaria. For the application of artesunate tablets, using a total amount of 0.28 g in 3d course of treatment and a total amount of 0.44 g in 5d course of treatment, wherein applying the total amount 0.44 g (equivalent to 8.8 mg/kg) in 5d course for treatment of falciparum malaria can lead to the protozoa recrudescence rate being as low as 4.4% after clinical curing of the patients with no significant toxicity and side effect and no decline in reticulocytes, clarifying that the patients have good tolerance on this dose. Oral administration has low toxicity and rapid efficacy and is more convenient and simple for applying. Applying 0.24 g/kg of artesunate for treatment of 72 cases of chloroquine-resistant falciparum malaria results in both the cooling time and asexual parasite clearance time being within 36 h and severely sicken patients being clinically cured. This clarifies that artesunate injection has many advantages including rapid insecticidal effect, short-term efficacy, safety, etc., it is suitable for the treatment and saving of patients with severe chloroquine-resistant falciparum malaria. Uses 1. It has a relative strong killing effect on the asexual body of plasmodium falciparum and can result in rapid control of malaria episodes. 2. It is a kind of anti-malarial drug. Description Artesunate (88495-63-0) is a semisynthetic derivative of the natural product artemisinin which is clinically useful for treatment of malaria and other parasitic diseases. Depolarizes mitochondrial membrane via generation of reactive oxygen species which disrupt the electron transport chain.1 Generation of mitochondrial ROS is dependent on RIP1.2 Inhibits TNFα-induced production of proinflammatory cytokines in human RA fibroblast-like synoviocytes.3 Displays cytotoxicity against a variety of cancer cells4 and cancer stem cells5. Chemical Properties Fine-White Crystalline Powder Uses Derivative of Artemisinin. Antimalarial Brand name Arsumax (Knoll, Switzerland). General Description Artesunate is a semisynthetic derivative of artemisinin used to treat malaria. It has also been shown to effective against other parasites such as liver flukes. Artesunate also demonstrates cytotoxic action against cancer cell lines of different tumor types. Biochem/physiol Actions Artesunate acts on the electron transport chain, generates local reactive oxygen species, and causes the depolarization of the mitochondrial membrane. It inhibits TNFα-induced production of proinflammatory cytokines via inhibition of NF-κB and PI3 kinase/Akt signal pathway in human rheumatoid arthritis fibroblast-like synoviocytes. References 1) Li et al. (2005), Yeast model uncovers dual roles of mitochondria in action of artemisinin; PLoS Genet., 1(3) e36 2) Chauhan et al. (2017), RIP1-dependent reactive oxygen species production executes artesunate-induced cell death in renal carcinoma Caki cells; Mol. Cell. Biochem., 435 15 3) Xu et al. (2007), Anti-malarial agent artesunate inhibits TNF-alpha-induced production of proinflammatory cytokines via inhibition of NF-kappaB and PI3 kinase/AKt signal pathway in human rheumatoid arthritis fibroblast-like synoviocytes; Rheumatology (Oxford), 46 920 4) Ghantous et al. (2010), What made sesquiterpene lactones reach cancer clinical trials ; Drug. Disc. Today, 15 668 5) Subedi et al. (2016), High-throughput screening identifies artesunate as selective inhibitor of cancer stemness: Involvement of mitochondrial metabolism; Biochem. Biophys. Res. Commun., 477 737   Artesunate Preparation Products And Raw materials Raw materials Succinic anhydride-->DHQHS 2-->alpha-Dihydroartemisinin Preparation Products Artemisinin

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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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Artesunate Basic information Antiparasitic drug Dosage and administration Clinical application Uses Product Name: Artesunate Synonyms: ARTENSUNATE;Butanedioic acid, 1-[(3R,5aS,6R,8aS,9R,10S,12R,12aR)-decahydro-3,6,9-trimethyl-3,12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin-10-yl] ester;Artesunate (3R,5aS,6R,8aS,9R,10S,12R,12aR)-Decahydro-3,6,9-trimethyl-3,12-epoxy-12H-pyrano(4,3-j)-1,2-benzodioxepin-10-ol hydrogen succinate;ARTESUNATE;ArtesunateC19H28O8;Artemisinin monosuccinate;Artesunic Acid;Butanedioic Acid Mono(3R,5aS,6R,8aS,9R,10R,12R,12aR)-decahydro-3,6,9-trimethyl-3,12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin-10-yl] Ester CAS: 88495-63-0 MF: C19H28O8 MW: 384.42 EINECS: 618-170-5 Product Categories: natural product;Antimalarial;Natural Plant Extract;plant extract;Herb extract;Inhibitors;Active Pharmaceutical Ingredients;Intermediates & Fine Chemicals;Pharmaceuticals;88495-63-0 Mol File: 88495-63-0.mol   Artesunate Chemical Properties Melting point  132-1350C Boiling point  431.1°C (rough estimate) density  1.2076 (rough estimate) refractive index  1.4430 (estimate) storage temp.  2-8°C solubility  acetone: soluble33.4mg/mL form  crystalline powder pka 4.28±0.17(Predicted) color  white to off-white Merck  14,818 Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.   Safety Information Hazard Codes  Xn Risk Statements  20/21/22 Safety Statements  24/25 WGK Germany  3 HS Code  29419090 Hazardous Substances Data 88495-63-0(Hazardous Substances Data) MSDS Information   Artesunate Usage And Synthesis Antiparasitic drug Artesunate is a kind of commonly used anti-parasitic drug and belongs to reduced artemisinin succinate monoester, and is the derivative of artemisinin containing a sesquiterpene lactone structure, and has a stronger efficacy on treating parasite than artemisinin and is also effective on treating chloroquine resistant strains. It acts on the Plasmodium schizonts on the erythrocytic stage. It takes effect by inhibiting cytochrome oxidase through reduced artemisinin to achievement of the inhibition on the function of cytochrome oxidase of malaria parasite surface membrane-food vacuole membrane, mitochondrial membrane, and thus blocking the supplying of nutrition from the host cell cytoplasm. It has a strong killing effect on the asexual form of plasmodium with a rapid efficacy enabling the rapid control of the onset of malaria. It has good efficacy on treating cerebral malaria, falciparum malaria and vivax malaria with similar efficacy in treating chloroquine-resistant strain of the falciparum malaria, especially with more significant effect on treating cerebral malaria. It can quickly control the emergence of malaria but has no effect on falciparum malaria gametophyte. It has a shorter T1/2 than artemether with blood concentration rapid decreasing after intravenous injection. Its T1/2 is about 30 min. It is widely distributed in the body with the content in intestine, liver, kidney being relative high. Urine and fecal excretion account for only a small fraction. It mainly undergoes metabolic conversion. It is clinically suitable for rescue of critically ill patients with acute malaria and can be used as the first-choice drug for the treatment of patients with cerebral malaria and a variety of dangerous malaria. But its shortcoming is the recrudescence rate. No adverse reactions have been observed at the recommended therapeutic dose; the application of large doses may cause a transient reduction of the outer peripheral reticulocyte which will return to normal level after stopping drug. Women within 2 months of pregnancy should be disabled. Whether it will cause teratogenicity demands further study. Dosage and administration Powder: 60mg; each artesunate is also attached with one 5% sodium bicarbonate injection. Upon application, first dissolve the drug in sodium bicarbonate injection, and then diluted to 10 ml with glucose injection after intravenous infusion at a rate of 3~4ml/min. For the treatment of patients of chloroquine-resistant falciparum malaria: 60 mg per time with the first dose being doubled; intravenously inject 1 times per day with 4 days as a course of treatment. The total dose is 300mg. When the symptom gets controlled, you can change with other anti-malarial drugs to reduce the recrudescence rate. The exact dosage and tablets should be according to the exact condition. The above information is edited by the Chemicalbook of Dai Xiongfeng. Clinical application The clinical application of artesunate has been as long as ten years. It is made through using the artemisia annua grass which is unique in China as raw material for extracting the active ingredient artemisinin and further going through chemical synthesis. Its major role is in treating plasmodia asexual form. It is also currently the only artemisinin derivatives which can be made into water-soluble formulation. It can be used to kill the parasite in inner phase of red blood cells to achieve the anti-malarial effect, and therefore being used in patients with various types of malaria, especially for treating and saving the patients with anti-chloroquine and anti-piperaquine falciparum malaria and severe-type cerebral malaria. It is characterized by high anti-malarial activity, high rate of fever abatement, short parasite clearance time and low drug toxic and side effects. It is the first-choice of drugs for the treatment of severe malaria. For the application of artesunate tablets, using a total amount of 0.28 g in 3d course of treatment and a total amount of 0.44 g in 5d course of treatment, wherein applying the total amount 0.44 g (equivalent to 8.8 mg/kg) in 5d course for treatment of falciparum malaria can lead to the protozoa recrudescence rate being as low as 4.4% after clinical curing of the patients with no significant toxicity and side effect and no decline in reticulocytes, clarifying that the patients have good tolerance on this dose. Oral administration has low toxicity and rapid efficacy and is more convenient and simple for applying. Applying 0.24 g/kg of artesunate for treatment of 72 cases of chloroquine-resistant falciparum malaria results in both the cooling time and asexual parasite clearance time being within 36 h and severely sicken patients being clinically cured. This clarifies that artesunate injection has many advantages including rapid insecticidal effect, short-term efficacy, safety, etc., it is suitable for the treatment and saving of patients with severe chloroquine-resistant falciparum malaria. Uses 1. It has a relative strong killing effect on the asexual body of plasmodium falciparum and can result in rapid control of malaria episodes. 2. It is a kind of anti-malarial drug. Description Artesunate (88495-63-0) is a semisynthetic derivative of the natural product artemisinin which is clinically useful for treatment of malaria and other parasitic diseases. Depolarizes mitochondrial membrane via generation of reactive oxygen species which disrupt the electron transport chain.1 Generation of mitochondrial ROS is dependent on RIP1.2 Inhibits TNFα-induced production of proinflammatory cytokines in human RA fibroblast-like synoviocytes.3 Displays cytotoxicity against a variety of cancer cells4 and cancer stem cells5. Chemical Properties Fine-White Crystalline Powder Uses Derivative of Artemisinin. Antimalarial Brand name Arsumax (Knoll, Switzerland). General Description Artesunate is a semisynthetic derivative of artemisinin used to treat malaria. It has also been shown to effective against other parasites such as liver flukes. Artesunate also demonstrates cytotoxic action against cancer cell lines of different tumor types. Biochem/physiol Actions Artesunate acts on the electron transport chain, generates local reactive oxygen species, and causes the depolarization of the mitochondrial membrane. It inhibits TNFα-induced production of proinflammatory cytokines via inhibition of NF-κB and PI3 kinase/Akt signal pathway in human rheumatoid arthritis fibroblast-like synoviocytes. References 1) Li et al. (2005), Yeast model uncovers dual roles of mitochondria in action of artemisinin; PLoS Genet., 1(3) e36 2) Chauhan et al. (2017), RIP1-dependent reactive oxygen species production executes artesunate-induced cell death in renal carcinoma Caki cells; Mol. Cell. Biochem., 435 15 3) Xu et al. (2007), Anti-malarial agent artesunate inhibits TNF-alpha-induced production of proinflammatory cytokines via inhibition of NF-kappaB and PI3 kinase/AKt signal pathway in human rheumatoid arthritis fibroblast-like synoviocytes; Rheumatology (Oxford), 46 920 4) Ghantous et al. (2010), What made sesquiterpene lactones reach cancer clinical trials ; Drug. Disc. Today, 15 668 5) Subedi et al. (2016), High-throughput screening identifies artesunate as selective inhibitor of cancer stemness: Involvement of mitochondrial metabolism; Biochem. Biophys. Res. Commun., 477 737   Artesunate Preparation Products And Raw materials Raw materials Succinic anhydride-->DHQHS 2-->alpha-Dihydroartemisinin Preparation Products Artemisinin