| Identification | Back Directory | [Name]
RO 9187 | [CAS]
876708-03-1 | [Synonyms]
RO 9187
RO 9187;RO9187
4-Amino-1-(4-C-azido-beta-D-arabinofuranosyl)-2(1H)-pyrimidinone | [Molecular Formula]
C9H12N6O5 | [MDL Number]
MFCD22665689 | [MOL File]
876708-03-1.mol | [Molecular Weight]
284.229 |
| Chemical Properties | Back Directory | [Melting point ]
188.0-189.0℃ | [storage temp. ]
Store at -20°C | [solubility ]
H2O : 7.14 mg/mL (25.12 mM; Need ultrasonic) | [form ]
Powder | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
RO-9187 is a potent inhibitor of HCV virus replication with an IC50 of 171 nM. RO-9187 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. | [Biological Activity]
RO-9187 is a potent inhibitor of HCV viral replication with IC50 value of 171 nM. | [in vitro]
RO-9187 is excellent substrates for deoxycytidine kinase and is phosphorylated with efficiencies up to 3-fold higher than deoxycytidine. It inhibits RNA synthesis by HCV polymerases from either HCV genotypes 1a and 1b or containing S96T or S282T point mutations with similar potencies, suggesting no cross-resistance with either R1479 (4′-azidocytidine) or 2′-C-methyl nucleosides. The formation of RO-9187-TP increased in a time- and dose-dependent manner. The maximal triphosphate concentration at 24 h is 87 pmol/106 cells with half-maximal triphosphate formation achieved at 12 μM RO-9187. | [in vivo]
Plasma exposures of RO-9187 in rats increase in a dose-dependent manner between 10 and 2000 mg/kg after oral dosing. Plasma concentrations of 1.4 and 26 μM (390 and 7454 ng/mL) are achieved in rats and dogs at the 10 mg/kg dose level, respectively. Plasma concentrations up to 57 μM are achieved in rats dosed with 2000 mg/kg/day. | [target]
| [References]
[1] Klumpp K, et al. 2'-deoxy-4'-azido nucleoside analogs are highly potent inhibitors of hepatitis C virus replication despite the lack of 2'-alpha-hydroxyl groups. J Biol Chem. 2008 Jan 25;283(4):2167-75. DOI:10.1074/jbc.M708929200 |
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| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
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