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  3. PSI-6130

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

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10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PSI-6130

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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]

Cellular Effect
Cell Line Type Value Description References
Huh-7 CC50
> 100 μM
Compound: 1
Cytotoxic concentration against HCV replication RNA levels in Huh7 cells determined by HCV replicon assay
Cytotoxic concentration against HCV replication RNA levels in Huh7 cells determined by HCV replicon assay
[PMID: 16107149]
Huh-7 CC50
> 50 μM
Compound: 1, PSI-6130
Cytotoxicity against human HuH7 cells by MTS assay
Cytotoxicity against human HuH7 cells by MTS assay
[PMID: 20580554]
Huh-7 CC50
> 98 μM
Compound: 9a, PSI-6130
Cytotoxicity against human HuH7 cells assessed as inhibition of cell proliferation after 3 days by BrdU incorporation assay
Cytotoxicity against human HuH7 cells assessed as inhibition of cell proliferation after 3 days by BrdU incorporation assay
[PMID: 24345201]
Huh-7 CC50
> 98.4 μM
Compound: 2, PSI-6130
Cytotoxicity against human HuH7 cells expressing CMV-Luc after 3 days by luciferase assay
Cytotoxicity against human HuH7 cells expressing CMV-Luc after 3 days by luciferase assay
[PMID: 21033671]
Huh-7 EC50
0.6 μM
Compound: 17
Antiviral activity against HCV genotype 1a infected in human HuH7 cells by replicon based assay
Antiviral activity against HCV genotype 1a infected in human HuH7 cells by replicon based assay
[PMID: 25650256]
Huh-7 EC50
0.61 μM
Compound: PSI-6130
Antiviral activity against Hepatitis C virus subtype 1b Con1 infected in human HuH7 cells after 3 days by luciferase reporter gene assay
Antiviral activity against Hepatitis C virus subtype 1b Con1 infected in human HuH7 cells after 3 days by luciferase reporter gene assay
[PMID: 18285474]
Huh-7 EC50
1.9 μM
Compound: 9a, PSI-6130
Antiviral activity against Hepatitis C virus genotype 1b in human Huh7-luc clone ET replicon cells assessed as inhibition of replicon replication after 3 days by luciferase assay
Antiviral activity against Hepatitis C virus genotype 1b in human Huh7-luc clone ET replicon cells assessed as inhibition of replicon replication after 3 days by luciferase assay
[PMID: 24345201]
Huh-7 EC50
1.9 μM
Compound: 2, PSI-6130
Antiviral activity against Hepatitis C virus subtype 1b with adaptive mutations of E1202G, T1280I, K1846T in NS5B polymerase infected in human HuH7 cells assessed as inhibition of viral replication after 3 days by luciferase assay
Antiviral activity against Hepatitis C virus subtype 1b with adaptive mutations of E1202G, T1280I, K1846T in NS5B polymerase infected in human HuH7 cells assessed as inhibition of viral replication after 3 days by luciferase assay
[PMID: 21033671]
Huh-7 EC50
2.3 μM
Compound: 17
Antiviral activity against HCV genotype 1b infected in human HuH7 cells by replicon based assay
Antiviral activity against HCV genotype 1b infected in human HuH7 cells by replicon based assay
[PMID: 25650256]
Huh-7 EC50
4.5 μM
Compound: PSI-6130
Antiviral activity against HCV infected in human Huh7 cells assessed as reduction in viral RNA replication after 4 days
Antiviral activity against HCV infected in human Huh7 cells assessed as reduction in viral RNA replication after 4 days
[PMID: 27994763]
MT4 CC50
> 98.4 μM
Compound: 2, PSI-6130
Cytotoxicity against human MT4 cells expressing LTR-Luc after 3 days by luciferase assay
Cytotoxicity against human MT4 cells expressing LTR-Luc after 3 days by luciferase assay
[PMID: 21033671]
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].

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

Molecular Weight

259.24

Formula

C10H14FN3O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N=C(C=CN1[C@@H]([C@@](C)([C@@H]2O)F)O[C@@H]2CO)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (96.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8575 mL 19.2874 mL 38.5747 mL
5 mM 0.7715 mL 3.8575 mL 7.7149 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.39%

References
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.8575 mL 19.2874 mL 38.5747 mL 96.4369 mL
5 mM 0.7715 mL 3.8575 mL 7.7149 mL 19.2874 mL
10 mM 0.3857 mL 1.9287 mL 3.8575 mL 9.6437 mL
15 mM 0.2572 mL 1.2858 mL 2.5716 mL 6.4291 mL
20 mM 0.1929 mL 0.9644 mL 1.9287 mL 4.8218 mL
25 mM 0.1543 mL 0.7715 mL 1.5430 mL 3.8575 mL
30 mM 0.1286 mL 0.6429 mL 1.2858 mL 3.2146 mL
40 mM 0.0964 mL 0.4822 mL 0.9644 mL 2.4109 mL
50 mM 0.0771 mL 0.3857 mL 0.7715 mL 1.9287 mL
60 mM 0.0643 mL 0.3215 mL 0.6429 mL 1.6073 mL
80 mM 0.0482 mL 0.2411 mL 0.4822 mL 1.2055 mL
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PSI-6130 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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