1. Anti-infection
    Metabolic Enzyme/Protease
  2. HCV
    HCV Protease

PSI-6130 (Synonyms: R 1656)

Cat. No.: HY-10165 Purity: 99.39%
Data Sheet SDS Handling Instructions

PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase, and inhibits HCV replication with a mean IC50 of 0.6 μM. 

For research use only. We do not sell to patients.
PSI-6130 Chemical Structure

PSI-6130 Chemical Structure

CAS No. : 817204-33-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 257 In-stock
2 mg USD 180 In-stock
5 mg USD 240 In-stock
10 mg USD 420 In-stock
50 mg USD 1188 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase, and inhibits HCV replication with a mean IC50 of 0.6 μM. 

IC50 & Target

IC50: 0.6 μM (HCV replication)[2]

In Vitro

PSI-6130 exhibits potent and specific inhibitory activity against HCV RNA replication mediated by the NS5B polymerase. Both PSI-6130 inhibit HCV GT-1b (Con1 strain) and GT-1a (H77 strain) subgenomic RNA replication, with mean EC50 values of 0.51 and 0.30 μM, respectively. PSI-6130 inhibits 40% human serum with EC50 of 0.51 μM[1]. PSI-6130 inhibits HCV replication with a mean IC50 of 0.6 μM, PSI-6130-TP inhibits HCV replicase with a mean IC50 of 0.34 μM. PSI-6130-TP inhibits 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 Ki of 0.023 μM[2].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 3.8576 mL 19.2879 mL 38.5758 mL
5 mM 0.7715 mL 3.8576 mL 7.7152 mL
10 mM 0.3858 mL 1.9288 mL 3.8576 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

The inhibition potency of compounds with respect to the RdRp activity of recombinant NS5B570-BK, NS5B570-Con1, and NS5B570-H77 proteins is determined by measuring the incorporation of radiolabeled NMP into acid-insoluble RNA products by use of a complement strand of internal ribosomal entry site (cIRES) RNA template. Briefly, 50% inhibitory concentration (IC50) determinations are carried out using 200 nM in vitro-transcribed cIRES RNA template, 1 μCi of tritiated UTP (42 Ci/mmol), 500 μM ATP, 500 μM GTP, 1 μM CTP, 1× TMDN buffer (40 mM Tris-HCl [pH 8.0], 4 mM MgCl2, 4 mM dithiothreitol, 40 mM NaCl), and 200 nM enzyme. The inhibition potency of compounds with respect to the RdRp activity of NS5B570-S282T-Con1 is determined under GT-1b assay conditions as. NS5B570-BK and NS5B570-Con1 enzymes are used as controls. The final reaction volume is 50 μL under all assay conditions. All reactions contain a final 10% dimethyl sulfoxide. Km and Ki values are measured. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

259.23

Formula

C₁₀H₁₄FN₃O₄

CAS No.

817204-33-4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.39%

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Product Name:
PSI-6130
Cat. No.:
HY-10165
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