Daclatasvir dihydrochloride - CAS 1009119-65-6
Catalog number: B0084-454273
Category: Inhibitor
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Daclatasvir is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture.
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B0084-454273 5 g $398 In stock
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Methyl N-[(2S)-1-[(2S)-2-[5-[4-[4-[2-[(2S)-1-[(2S)-2-(methoxycarbonylamino)-3-methylbutanoyl]pyrrolidin-2-yl]-1H-imidazol-5-yl]phenyl]phenyl]-1H-imidazol-2-yl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]carbamate dihydrochloride; Daclatasvir; BMS790052; BMS 790052; BMS-790052; EBP883; EBP 883; EBP-883; Daklinza
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1.Synthesis of isotopically labeled daclatasvir for use in human clinical studies.
Easter JA;Burrell RC;Bonacorsi SJ Jr J Labelled Comp Radiopharm. 2016 Apr;59(4):164-70. doi: 10.1002/jlcr.3386. Epub 2016 Mar 10.
Daclatasvir is a novel hepatitis C virus NS5A inhibitor developed by Bristol-Myers Squibb and marketed as Daklinza®. The need to support the development of daclatasvir required the synthesis of carbon-14 labeled material for use in human absorption, distribution, metabolism, and excretion studies. A total of 7.53 mCi of [(14) C]-daclatasvir was synthesized in eight steps from commercially available [(14) C]-copper cyanide. The radiochemical purity was 99.6%, and specific activity was 3.86 μCi/mg. To support a human absolute bioavailability study, 5.56 g of [(13) C2 , (15) N4 ]-daclatasvir was synthesized in four steps.
2.Daclatasvir: A Review in Chronic Hepatitis C.
Keating GM Drugs. 2016 Sep;76(14):1381-91. doi: 10.1007/s40265-016-0632-x.
The hepatitis C virus (HCV) NS5A replication complex inhibitor daclatasvir (Daklinza(®)) is indicated for use in combination with sofosbuvir, with or without ribavirin, in a pangenotypic all-oral regimen. In patients with chronic HCV genotype 1 or 3 infection without cirrhosis, a 12-week regimen of daclatasvir plus sofosbuvir achieved high sustained virological response rates 12 weeks' post-treatment (SVR12), regardless of prior treatment experience, according to the results of the AI444040 and ALLY-3 trials. In the ALLY-3+ trial, high SVR12 rates were achieved with a 12- or 16-week regimen of daclatasvir plus sofosbuvir and ribavirin in patients with chronic HCV genotype 3 infection and advanced fibrosis or compensated cirrhosis. A daclatasvir plus sofosbuvir-based regimen demonstrated efficacy in patients with chronic HCV genotype 1, 3 or 4 infection and advanced cirrhosis or post-transplant recurrence in the ALLY-1 trial, and in patients co-infected with HCV genotype 1, 3 or 4 and HIV-1 in the ALLY-2 trial. Results of clinical trials were supported by real-world data from early-access programmes that included high numbers of patients who would have been excluded from phase 3 trials because of advanced disease and/or concomitant medical conditions.
3.Pharmaceutical Approval Update.
Gohil K P T. 2015 Oct;40(10):649-89.
Alirocumab (Praluent) for high cholesterol; flibanserin (Addyi) for sexual desire disorder in women; daclatasvir (Daklinza) for chronic hepatitis C virus (HCV) genotype 3 infection; and ombitasvir/paritaprevir/ritonavir (Technivie) for genotype 4 HCV infection without cirrhosis.
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CAS 1009119-65-6 Daclatasvir dihydrochloride

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