N-[[P(S),2'R]-2'-Deoxy-2'-fluoro-2'-Methyl-6-O-Methyl-P-phenyl-5'-guanylyl]- L-alanine 1-Methylethyl ester
- Product Name
- N-[[P(S),2'R]-2'-Deoxy-2'-fluoro-2'-Methyl-6-O-Methyl-P-phenyl-5'-guanylyl]- L-alanine 1-Methylethyl ester
- CAS No.
- 1231747-08-2
- Chemical Name
- N-[[P(S),2'R]-2'-Deoxy-2'-fluoro-2'-Methyl-6-O-Methyl-P-phenyl-5'-guanylyl]- L-alanine 1-Methylethyl ester
- Synonyms
- PSI-353661;N-[[P(S),2'R]-2'-Deoxy-2'-fluoro-2'-Methyl-6-O-Methyl-P-phenyl-5'-guanylyl]- L-alanine 1-Methylethyl ester;L-Alanine, N-[[P(S),2'R]-2'-deoxy-2'-fluoro-2'-methyl-6-O-methyl-P-phenyl-5'-guanylyl]-, 1-methylethyl ester;N-[[P(S),2'R]-2'-Deoxy-2'-fluoro-2'-Methyl-6-O-Methyl-P-phenyl-5'-guanylyl]- L-alanine 1-Methylethyl ester USP/EP/BP
- CBNumber
- CB52604355
- Molecular Formula
- C24H32FN6O8P
- Formula Weight
- 582.52
- MOL File
- 1231747-08-2.mol
N-[[P(S),2'R]-2'-Deoxy-2'-fluoro-2'-Methyl-6-O-Methyl-P-phenyl-5'-guanylyl]- L-alanine 1-Methylethyl ester Property
- Density
- 1.53
N-Bromosuccinimide Price
- Product number
- INB0001533
- Product name
- PSI-353661
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $496.83
- Updated
- 2021/12/16
N-[[P(S),2'R]-2'-Deoxy-2'-fluoro-2'-Methyl-6-O-Methyl-P-phenyl-5'-guanylyl]- L-alanine 1-Methylethyl ester Chemical Properties,Usage,Production
Uses
PSI-353661 (GS-558093) is a purine nucleotide NS5B polymerase inhibitor against HCV infection. PSI-353661 shows EC90s of 8 nM and 11 nM for wild type and S282T resistant replicons of HCV. PSI-353661 can produce high concentrations of the active triphosphate in primary human hepatocytes[1][3].
in vivo
PSI-353661 (50 mg/kg, p.o., together with 400 mg/kg of Telaprevir.html" class="link-product" target="_blank">Telaprevir (HY-10235), daily for 4 weeks) is effective against human hepatocyte chimeric mice infected with HCV[3].
| Animal Model: | Human hepatocyte chimeric mice infected with HCV |
| Dosage: | 50 mg/kg, together with 400 mg/kg of Telaprevir |
| Administration: | Oral administration (p.o.) |
| Result: | Achieved sustained eradication of the mutant virus or the end-of-treatment response. Reduced serum levels of HCV RNA. |
References
[1] Wonsuk Chang, et al. Discovery of PSI-353661, a Novel Purine Nucleotide Prodrug for the Treatment of HCV Infection. ACS Med Chem Lett. 2010 Dec 17;2(2):130-5. DOI:10.1021/ml100209f
[2] Furman PA, et al. Activity and the metabolic activation pathway of the potent and selective hepatitis C virus pronucleotide inhibitor PSI-353661. Antiviral Res. 2011 Aug;91(2):120-32. DOI:10.1016/j.antiviral.2011.05.003
[3] Yugo Kai, et al. Emergence of hepatitis C virus NS5A L31V plus Y93H variant upon treatment failure of daclatasvir and asunaprevir is relatively resistant to ledipasvir and NS5B polymerase nucleotide inhibitor GS-558093 in human hepatocyte chimeric mice. DOI:10.1007/s00535-015-1108-6
N-[[P(S),2'R]-2'-Deoxy-2'-fluoro-2'-Methyl-6-O-Methyl-P-phenyl-5'-guanylyl]- L-alanine 1-Methylethyl ester Preparation Products And Raw materials
Raw materials
Preparation Products
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