1. Cell Cycle/DNA Damage Anti-infection Metabolic Enzyme/Protease
  2. DNA/RNA Synthesis SARS-CoV RSV HCV Drug Metabolite
  3. GS-443902 trisodium

GS-443902 trisodium  (Synonyms: GS-441524 triphosphate trisodium; Remdesivir metabolite trisodium)

Cat. No.: HY-126303C Pureza: 99.94%
Instrucciones de manejo Technical Support

GS-443902 trisodium (GS-441524 triphosphate trisodium) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC50s of 1.1 μM, 5 μM for RSV RdRp and HCV RdRp, respectively. GS-443902 trisodium is the active triphosphate metabolite of Remdesivir (GS-5734).

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GS-443902 trisodium

GS-443902 trisodium Estructura química

No. CAS : 1355050-21-3

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Revisión del cliente

Based on 13 publication(s) in Google Scholar

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Descripciòn

GS-443902 trisodium (GS-441524 triphosphate trisodium) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC50s of 1.1 μM, 5 μM for RSV RdRp and HCV RdRp, respectively. GS-443902 trisodium is the active triphosphate metabolite of Remdesivir (GS-5734)[1][2].

IC50 & Target

IC50: 1.1 μM (RSV RdRp) and 5 μM (HCV RdRp)[1][2]

In Vitro

In a continuous 72 h incubation of 1 μM Remdesivir (GS-5734), the GS-443902 trisodium (GS-441524 triphosphate trisodium; Remdesivir metabolite trisodium) level is measured at 2, 24, 48 and 72 h, and reaches a Cmax of 300, 110, and 90 pmol/million cells in macrophages, HMVEC, and HeLa cells lines respectively[1].
GS-443902 trisodium (compound 8a) is a triphosphates (TP) derivative[2].
GS-443902 trisodium (NTP; 0.01, 0.1, 1, 10, 100 μM) inhibits RSV RdRp-catalysed RNA synthesis by incorporating into the nascent viral RNA transcript and causing its premature termination. GS-5734 selectively inhibits EBOV replication by targeting its RdRp and inhibiting viral RNA synthesis following efficient intracellular conversion to GS-443902 sodium[3].

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

In Vivo

Remdesivir (GS-5734; 10 mg kg; i.v.) rapidly distributes into peripheral blood mononuclear cells (PBMCs), and efficient conversion to GS-443902 trisodium (Remdesivir metabolite trisodium; NTP) is apparent within 2 h of dose administration in rhesus monkeys. In PBMCs, GS-443902 trisodium represents the predominant metabolite and is persistent with a t1/2 of 14 h and levels required for >50% virus inhibition for 24 hours[3].

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

Peso molecular

597.15

Fòrmula

C12H13N5Na3O13P3

No. CAS
Appearance

Solid

Color

White to light yellow

SMILES

O=P(OP(O)(O[Na])=O)(O[Na])OP(OC[C@@H](O1)[C@@H](O)[C@@H](O)[C@]1(C#N)C2=CC=C3N2N=CN=C3N)(O[Na])=O

Envío

Shipping with dry ice.

Almacenamiento

-80°C, protect from light, stored under nitrogen

*The compound is unstable in solutions, freshly prepared is recommended.

Solvente y solubilidad
In Vitro: 

H2O : 33.33 mg/mL (55.82 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6746 mL 8.3731 mL 16.7462 mL
5 mM 0.3349 mL 1.6746 mL 3.3492 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

* 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.

  • Calculadora de molaridad

  • Calculadora de dilución

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:

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: 50 mg/mL (83.73 mM); Clear solution; Need ultrasonic

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.
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).
Pureza y Documentación

Purity: 99.94%

Referencias

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 1.6746 mL 8.3731 mL 16.7462 mL 41.8655 mL
5 mM 0.3349 mL 1.6746 mL 3.3492 mL 8.3731 mL
10 mM 0.1675 mL 0.8373 mL 1.6746 mL 4.1866 mL
15 mM 0.1116 mL 0.5582 mL 1.1164 mL 2.7910 mL
20 mM 0.0837 mL 0.4187 mL 0.8373 mL 2.0933 mL
25 mM 0.0670 mL 0.3349 mL 0.6698 mL 1.6746 mL
30 mM 0.0558 mL 0.2791 mL 0.5582 mL 1.3955 mL
40 mM 0.0419 mL 0.2093 mL 0.4187 mL 1.0466 mL
50 mM 0.0335 mL 0.1675 mL 0.3349 mL 0.8373 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.

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Nombre del producto:
GS-443902 trisodium
Cat. No.:
HY-126303C
Cantidad:
MCE Japan Authorized Agent: