PSI-7409 tetrasodium

Name: PSI-7409 tetrasodium
Brand: MedChemExpress
SKU: HY-15745A
Rating: 5.0 (6 reviews)

Cat. No.: HY-15745A Purity: 99.31%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 1621884-22-7

Size	Price	Stock	Quantity
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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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of PSI-7409 tetrasodium:

PSI-7409 In-stock

6 Publications Citing Use of MCE PSI-7409 tetrasodium

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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].

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

Molecular Weight

588.09

Formula

C₁₀H₁₂FN₂Na₄O₁₄P₃

CAS No.

1621884-22-7

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : ≥ 100 mg/mL (170.04 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7004 mL	8.5021 mL	17.0042 mL
5 mM	0.3401 mL	1.7004 mL	3.4008 mL
10 mM	0.1700 mL	0.8502 mL	1.7004 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (170.04 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.31%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (251 KB) HNMR (515 KB) CNMR (1169 KB) RP-HPLC (258 KB) MS (70 KB)

Handling Instructions (2659 KB)

References

[1]. Lam AM, et al. PSI-7851, a pronucleotide of beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine monophosphate, is a potent and pan-genotype inhibitor of hepatitis C virus replication. Antimicrob Agents Chemother. 2010 Aug;54(8):3187-96. [Content Brief]

[2]. Murakami E, et al. Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977. J Biol Chem. 2010 Nov 5;285(45):34337-47. [Content Brief]

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

[1]. Lam AM, et al. PSI-7851, a pronucleotide of beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine monophosphate, is a potent and pan-genotype inhibitor of hepatitis C virus replication. Antimicrob Agents Chemother. 2010 Aug;54(8):3187-96. [Content Brief]

[2]. Murakami E, et al. Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977. J Biol Chem. 2010 Nov 5;285(45):34337-47. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	1.7004 mL	8.5021 mL	17.0042 mL	42.5105 mL
	5 mM	0.3401 mL	1.7004 mL	3.4008 mL	8.5021 mL
	10 mM	0.1700 mL	0.8502 mL	1.7004 mL	4.2510 mL
	15 mM	0.1134 mL	0.5668 mL	1.1336 mL	2.8340 mL
	20 mM	0.0850 mL	0.4251 mL	0.8502 mL	2.1255 mL
	25 mM	0.0680 mL	0.3401 mL	0.6802 mL	1.7004 mL
	30 mM	0.0567 mL	0.2834 mL	0.5668 mL	1.4170 mL
	40 mM	0.0425 mL	0.2126 mL	0.4251 mL	1.0628 mL
	50 mM	0.0340 mL	0.1700 mL	0.3401 mL	0.8502 mL
	60 mM	0.0283 mL	0.1417 mL	0.2834 mL	0.7085 mL
	80 mM	0.0213 mL	0.1063 mL	0.2126 mL	0.5314 mL
	100 mM	0.0170 mL	0.0850 mL	0.1700 mL	0.4251 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.