产品说明书

PSI-6130

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Chemical Structure| 817204-33-4 同义名 : R 1656
CAS号 : 817204-33-4
货号 : A669372
分子式 : C10H14FN3O4
纯度 : 98%
分子量 : 259.234
MDL号 : MFCD13176566
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(96.44 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 PSI-6130 demonstrates effective and specific inhibitory activity against HCV RNA replication mediated by the NS5B polymerase. PSI-6130 inhibits subgenomic RNA replication of both HCV GT-1b (Con1 strain) and GT-1a (H77 strain), with average EC50 values of 0.51 μM and 0.30 μM, respectively. In the presence of 40% human serum, PSI-6130 maintains its inhibitory effect with an EC50 of 0.51 μM[1]. PSI-6130 inhibits HCV replication with an average IC50 of 0.6 μM, while PSI-6130-TP inhibits the HCV replicase with an average IC50 of 0.34 μM. PSI-6130-TP also inhibits the recombinant HCV Con1 NS5B on a heteropolymeric RNA template derived from the 3' end of the negative strand of the HCV genome, with an IC50 of 0.13 μM and a Ki of 0.023 μM[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.86mL

0.77mL

0.39mL

19.29mL

3.86mL

1.93mL

38.58mL

7.72mL

3.86mL
参考文献

[1]Ali S, et al. Selected replicon variants with low-level in vitro resistance to the hepatitis C virus NS5B polymerase inhibitor PSI-6130 lack cross-resistance with R1479. Antimicrob Agents Chemother. 2008 Dec;52(12):4356-69.

[2]Ma H, et al. Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. J Biol Chem. 2007 Oct 12;282(41):298