1. Anti-infection
  2. HCV

PSI-7409 tetrasodium 

Cat. No.: HY-15745A Purity: 96.49%
Handling Instructions

PSI-7409 tetrasodium is an active 5'-triphosphate metabolite of sofosbuvir (PSI-7977), inhibiting HCV NS5B polymerases, with IC50s of 1.6, 2.8, 0.7 and 2.6 μM for GT 1b_Con1, GT 2a_JFH1, GT 3a, and GT 4a NS5B polymerases, respectively.

For research use only. We do not sell to patients.

PSI-7409 tetrasodium Chemical Structure

PSI-7409 tetrasodium Chemical Structure

CAS No. : 1621884-22-7

Size Price Stock Quantity
10 mM * 1 mL in Water USD 1016 In-stock
Estimated Time of Arrival: December 31
1 mg USD 260 In-stock
Estimated Time of Arrival: December 31
5 mg USD 780 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2400 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Other Forms of PSI-7409 tetrasodium:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

PSI-7409 tetrasodium is an active 5'-triphosphate metabolite of sofosbuvir (PSI-7977), inhibiting HCV NS5B polymerases, with IC50s of 1.6, 2.8, 0.7 and 2.6 μM for GT 1b_Con1, GT 2a_JFH1, GT 3a, and GT 4a NS5B polymerases, respectively.

IC50 & Target

IC50: 1.6 μM (GT 1b_Con1), 2.8 μM (GT 2a_JFH1), 0.7 μM (GT 3a), 2.6 μM (GT 4a)[1]

In Vitro

PSI-7409 tetrasodium is an active 5'-triphosphate metabolite, inhibiting HCV NS5B polymerases, with IC50s of 1.6, 2.8, 0.7 and 2.6 μM for GT 1b_Con1, GT 2a_JFH1, GT 3a, and GT 4a NS5B polymerases, respectively. PSI-7409 also weakly inhibits human DNA polymerase α, with an IC50 of 550 μM, but shows no inhibition on DNA Pol β and γ[1]. In clone A cells, the levels of PSI-7409 gradually increases to a maximum concentration of about 25 μM over a period of 48 h. PSI-7409 forms at a much faster rate in primary human hepatocytes, achieving a maximum intracellular concentration of ∼100 μM at 4 h and remains at that concentration for 48 h[2].

Solvent & Solubility
In Vitro: 

H2O : ≥ 125 mg/mL (211.11 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6888 mL 8.4442 mL 16.8885 mL
5 mM 0.3378 mL 1.6888 mL 3.3777 mL
10 mM 0.1689 mL 0.8444 mL 1.6888 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Human DNA polymerase α, β, or γ is assayed in a 10-μL reaction mixture containing 50 mM Tris (pH 7.5), 50 mM NaCl, 3 mU/μL activated calf thymus DNA, a 20 μM concentration of all four natural deoxynucleoside triphosphates, 4 μCi [α-32P]dCTP, 5 mM MgCl2, and increasing concentrations of PSI-7409 (up to 1 mM), D-ddFCTP, or aphidicolin. DNA polymerase α, β, or γ is added to the reaction mixture to give final concentrations of 20, 18, and, 50 μg/mL, respectively. All reactions are run at 37°C and quenched at 30 min by mixing with 1 μL of 0.5 M EDTA. The radiolabeled products are quantified. A nonlinear fit is performed to determine the IC50. The activity of RNA polymerase II is determined in a 25-μL in vitro transcription reaction mixture containing 100 ng of cytomegalovirus (CMV) immediate-early promoter DNA, 400 μM ATP, CTP, and UTP, 16 μM GTP, 10 μCi [α-32P]GTP, 3 mM MgCl2, and various concentrations of PSI-7409 (up to 1 mM), 3'-dCTP, or α-amanitin in transcription buffer (20 mM HEPES [pH 7.9], 100 mM KCl, 0.2 mM EDTA, 0.5 mM DTT, and 20% glycerol). All reactions are run at 30°C and quenched at 60 min by mixing with 125 μL of stop solution (0.3 M Tris-HCl [pH 7.4], 0.3 M sodium acetate, 0.5% SDS, 2 mM EDTA, and 3 μg/mL tRNA). The RNA product is purified. The resulting samples contains 12 μL and the same volume of gel loading dye (98% formamide, 10 mM EDTA, 0.1% xylene cyanol, and 0.1% bromophenol blue) is added. The samples are heated at 90°C for 5 min and loaded onto a 6% polyacrylamide sequencing gel. After running, the gel is exposed to a phosphorscreen, and the product is visualized and quantified by using a phosphorimager[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

592.12

Formula

C₁₀H₁₆FN₂Na₄O₁₄P₃

CAS No.

1621884-22-7

SMILES

O[[email protected]@H]([[email protected]@](C)(F)[[email protected]](N1C(NC(C=C1)=O)=O)O2)[[email protected]]2COP(O)(OP(OP(O)(O)=O)(O)=O)=O.[4Na]

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

Room temperature in continental US; may vary elsewhere

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Product Name:
PSI-7409 tetrasodium
Cat. No.:
HY-15745A
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PSI-7409 tetrasodium

Cat. No.: HY-15745A