PSI-6130 (Synonyms: R 1656)

Name: PSI-6130
Brand: MedChemExpress
SKU: HY-10165
Rating: 4.5 (1 reviews)

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

COA
Handling Instructions Technical Support

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

CAS No. : 817204-33-4

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE PSI-6130

•Antiviral Res. 2019 Oct;170:104570. [Abstract]

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Biological Activity
Protocol
Purity & Documentation
References
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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 K_i 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.

817204-33-4

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
10 mM	0.3857 mL	1.9287 mL	3.8575 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (249 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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):29812-20. Epub 2007 Aug 13. [Content Brief]

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. K_m and K_i values are measured.

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

References

[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. [Content Brief]

[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):29812-20. Epub 2007 Aug 13. [Content Brief]

Complete Stock Solution Preparation Table

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

PSI-6130 Related Classifications

Infection

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.

Keywords:

PSI-6130817204-33-4R 1656PSI6130PSI 6130R1656R-1656HCVHepatitis C virusInhibitorinhibitorinhibit

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PSI-6130 (Synonyms: R 1656)

Customer Review

PSI-6130 Related Antibodies

1 Publications Citing Use of MCE PSI-6130

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

PSI-6130 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

PSI-6130 Related Classifications

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