Fialuridine Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Fialuridine (FIAU) is one of a series of 2'-fluoro-substituted arabinosyl pyrimidine nucleosides that have demonstrated potent antiviral activities against a number of clinically important viruses, including hepatitis B virus (HBV). Analogs of FIAU have been shown to inhibit viral replication in the woodchuck and duck models of HBV infection. Although the mechanism of the anti-HBV activity is not well understood, evidence suggests that the triphosphate analog of FIAU is a potent inhibitor of HBV DNA polymerase activity. During early clinical investigation FIAU showed much promise as an antiHBV drug because it markedly reduced the level of HBV DNA in the serum of patients with chronic hepatitis B. However, clinical trials were terminated after adverse events occurred following oral administration of FIAU (0.1 and 0.25 mg/kg of body weight per day) for more than 2 months. The mechanism of the unexpected delayed toxicity is unresolved.

Chemische Eigenschaften

Colourless crystals

Verwenden

Fialuridine has been used in the selection of clones.

Allgemeine Beschreibung

Fialuridine (1-(2-deoxy-2-fluoro-β-d-arabinofuranosyl)-5-iodouracil, or FIAU) is an antiviral agent. It is a thymidine-based nucleoside analogue.

Clinical Use

Fialuridine, a nucleoside analog designed for the treatment of hepatitis B virus infection, failed in clinical trials due to fatal hepatotoxicity, occuring after 13 weeks of 0.25 mg/kg qd dosing in HBV infected patients. Both in vitro assays as well as preclinical in vivo tests in mice, rats, dogs, and primates could not predict its hepatotoxic potential. Fialuridine toxicity is thought to be mediated by human-specific impaired mitochondrial function after long-term exposure. We used the micropatterned primary hepatocyte coculture model, HepatoPac™, to assess fialuridine-mediated toxicity in vitro. To confirm the human specific toxicity, also rat, dog and monkey HepatoPac™ were exposed to fialuridine.
Another nucleoside analog, sofosbuvir, which is on the market for the treatment of hepatitis C virus infection and shows no signs of hepatotoxicity in the clinic, was used to study whether this approach would be able to distinguish a nucleoside analog with clinical chronic DILI finding from a nucleoside analog without DILI findings.

Fialuridine Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

Fialuridine Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
career henan chemical co	+86-0371-86658258 +8613203830695	sales@coreychem.com	China	29880	58
Shenzhen Nexconn Pharmatechs Ltd	+86-755-89396905 +86-15013857715	admin@nexconn.com	China	10311	58
Nanjing Baifuli Technology Co., Ltd.	+86-15335185688	sales@unisyn.cn	CHINA	332	58
Hubei xin bonus chemical co. LTD	86-13657291602	linda@hubeijusheng.com	CHINA	22963	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19553	58
Chongqing Chemdad Co., Ltd	+86-023-6139-8061 +86-86-13650506873	sales@chemdad.com	China	39894	58
CONIER CHEM AND PHARMA LIMITED	+8618523575427	sales@conier.com	China	49374	58
SHANGHAI T&W PHARMACEUTICAL CO., LTD.	+86-021-61551413 +8618813727289	contact@trustwe.com	China	5738	58
Guangzhou Yuheng Pharmaceutical Technology Co., Ltd	+8613580539051	joe@yuhengpharm.com	CHINA	21142	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	32161	58

69123-98-4()Verwandte Suche:

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• 1-(2-deoxy-2-fluoro-beta-d-arabinofuranosyl)-5-iodouracil
• 2,4(1h,3h)-pyrimidinedione,1-(2-deoxy-2-fluoro-beta-d-arabinofuranosyl)-5-io
• 2’-fluoro-5-iodo-1-beta-d-arabinofuranosyluracil
• 2'-Deoxy-2'-fluoro-5-iodo-D-uridine
• 5-IODO-2'-FLUORO-2'-DEOXY-1-BETA-D-ARABINOFURANOSYLURACIL
• 2,4(1H,3H)-PYRIMIDINEDIONE, 1-(2-DEOXY-2-FLUORO-BETA-D-ARABINOFURANOSYL)-5-IODO-
• 2'-FLUORO-5-IODOURACIL
• 2'-FLUORO 2'-DEOXY-5-IODOURACIL-BETA-D-ARABINOFURANOSIDE
• 1-(2'FLUORO-2'-DEOXYARABINOFURANOSYL)-5-IODOURACIL
• 1-(2-DEOXY-2-FLUORO-B-D-ARABINOFURANOSYL)-5-IODOURACIL
• FIALURIDINE
• FIAU
• 1-[(2R,3S,4R,5R)-3-Fluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-iodopyrimidine-2,4-dione
• Fialuridine(FIAU)
• 5-Iodo-2'-fluoro-deoxyuridine
• 1-(2-deoxy-2-fluoro-beta-d-arabinofuranosyl)-5-iodo-uraci
• 2,4(1H,3H)-Pyrimidinedione, 1-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-5-iodo-
• 1-(2-Deoxy-2-fluoro-beta-D-arabinofuranosyl)-5-iodouracil 5-Iodo-2'-fluoroarauracil
• Fluoroiodoarauracil
• NSC 678514
• 1-(2-Deoxy-2-fluoro--D-arabinofuranosyl)-5-iodo-2,4(1H,3H)-pyrimidinedione
• 1-(2'-Deoxy-2'-fluoro--D-arabinofuranosyl)-5-iodouracil
• 5-Iodo-2'-fluoroarauracil
• 5-Iodo-1-(2-fluoro-2-deoxy-β-D-arabinofuranosyl)uracil
• 2'-Deoxy-2'-fluoro-5-iodouridine
• 5-Iodo-2'-fluoro-2'-deoxy-ara-uridine
• 1-(2-Deoxy-2-fluoro-β-D-arabinofuranosyl)-5-iodo-
• Fialuridine FIAU 2'-Fluoro-5-iodoarauracil
• 5-Iodo-2'-deoxy-2'-fluoro-beta-D-arabinouridine
• 5-I-2'-F-dU
• 1-[(2R,3S,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-iodo-1,2,3,4-tetrahydropyrimidine-2,4-dione
• 5-I-Ara-2'-F-2'-dU
• 1-(2-Deoxy-2-fluoro--D-arabinofuranosyl)-5-iodouracil (FIAU
• 1-(2-Deoxy-2-fluoro-β-D-arabinofuranosyl)-5-iodouracil>
• DRG-0098
• 5-Iodo-2’-deoxy-2’-fluoro-beta-D-arabinouridine, FIAU, Fiauridine
• 5-Iodo-2’-deoxy-2’-fluoro-β-D-arabinouridine
• 69123-98-4 1-(2-Deoxy-2-fluoro-β-D-arabinofuranosyl)-5-iodouracil
• 2'-Fluoro-5-iodoarauracil
• Fialuridine USP/EP/BP
• 1-(2-Deoxy-2-fluoro-β-D-arabinofuranosyl)-5-iodouracil
• 1-((2R,3S,4R,5R)-3-Fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-iodopyrimidine-2,4(1H,3H)-dione
• 5-Iodo-2’-deoxy-2’-fluoro-arabinouridine
• 5-1-Ara-2'-F-2-dU
• Fluoroiodoarauridine
• 5-Iodo-2’-deoxy-2’-fluoro-arabinouridine
• 5-1-Ara-2'-F-2-dU
• 69123-98-4
• C9H10FIN2O5
• Anti-virals
• Bases & Related Reagents
• Intermediates & Fine Chemicals
• Nucleotides
• Pharmaceuticals