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

Cat. No.: HY-126303: FAQs
Data Sheet SDS COA Handling Instructions

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GS-443902 (GS-441524 triphosphate) 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 is the active triphosphate metabolite of Remdesivir.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (GS-443902 trisodium) that retains the same biological activity.

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

GS-443902 Chemical Structure

CAS No. : 1355149-45-9

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Other Forms of GS-443902:

Remdesivir In-stock
GS-441524 Get quote
GS-443902 sodium Get quote
GS-443902 TEA Get quote
GS-443902 trisodium Get quote

10 Publications Citing Use of MCE GS-443902

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	> 200 μM Compound: 4tp	Inhibition of RNA polymerase 2 in human HeLa cells preincubated for 5 mins with dATP/dGTP/dTTP as substrate followed by addition of cell extract measured after 1 hr by SDS-PAGE method Inhibition of RNA polymerase 2 in human HeLa cells preincubated for 5 mins with dATP/dGTP/dTTP as substrate followed by addition of cell extract measured after 1 hr by SDS-PAGE method	[PMID: 28124907]

In Vitro

In a continuous 72 h incubation of 1 µM Remdesivir (GS-5734), the GS-443902 (GS-441524 triphosphate; Remdesivir metabolite; compound 4tp) level is measured at 2, 24, 48 and 72 h, and reaches a C_max of 300, 110, and 90 pmol/million cells in macrophages, HMVEC, and HeLa cells lines respectively^[1].
GS-443902 (compound 8a) is a triphosphates (TP) derivative^[2].
GS-443902 (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^[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 (GS-441524 triphosphate; Remdesivir metabolite; NTP) is apparent within 2 h of dose administration in rhesus monkeys. In PBMCs, GS-443902 represents the predominant metabolite and is persistent with a t_1/2 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.

Molecular Weight

531.20

Formula

C₁₂H₁₆N₅O₁₃P₃

CAS No.

1355149-45-9

Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

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

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (188.25 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8825 mL	9.4127 mL	18.8253 mL
5 mM	0.3765 mL	1.8825 mL	3.7651 mL
10 mM	0.1883 mL	0.9413 mL	1.8825 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.

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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

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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.

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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: 99.87%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (251 KB) HNMR (249 KB) LCMS (138 KB)

Handling Instructions (2659 KB)

References

[1]. Siegel D, et al. Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses. Med Chem. 2017 Mar 9;60(5):1648-1661. [Content Brief]

[2]. Cho A, et al. Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2705-7. [Content Brief]

[3]. Warren TK, et al. Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys. Nature. 2016 Mar 17;531(7594):381-5. [Content Brief]

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	1.8825 mL	9.4127 mL	18.8253 mL	47.0633 mL
	5 mM	0.3765 mL	1.8825 mL	3.7651 mL	9.4127 mL
	10 mM	0.1883 mL	0.9413 mL	1.8825 mL	4.7063 mL
	15 mM	0.1255 mL	0.6275 mL	1.2550 mL	3.1376 mL
	20 mM	0.0941 mL	0.4706 mL	0.9413 mL	2.3532 mL
	25 mM	0.0753 mL	0.3765 mL	0.7530 mL	1.8825 mL
	30 mM	0.0628 mL	0.3138 mL	0.6275 mL	1.5688 mL
	40 mM	0.0471 mL	0.2353 mL	0.4706 mL	1.1766 mL
	50 mM	0.0377 mL	0.1883 mL	0.3765 mL	0.9413 mL
	60 mM	0.0314 mL	0.1569 mL	0.3138 mL	0.7844 mL
	80 mM	0.0235 mL	0.1177 mL	0.2353 mL	0.5883 mL
	100 mM	0.0188 mL	0.0941 mL	0.1883 mL	0.4706 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.

GS-443902 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.

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