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

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

製品番号: HY-126303
COA 取扱説明書 Technical Support

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.

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GS-443902

GS-443902 構造式

CAS 番号 : 1355149-45-9

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GS-443902 関連抗体

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製品説明

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[1][2].

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]
体外実験

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 Cmax 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.

GS-443902 関連抗体
体内実験

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 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.
分子量

531.20

分子式

C12H16N5O13P3
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

-20°C, stored under nitrogen

*The compound is unstable in solutions, freshly prepared is recommended.
溶剤 & 溶解度
体外: 

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.

  • Molarity Calculator

  • Dilution Calculator

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

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

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体積 （開始）

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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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).
純度とドキュメンテーション

純度: 99.87%

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

取扱説明書 (2659 KB)
参考文献

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.

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GS-443902 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

GS-4439021355149-45-9GS-441524 triphosphate Remdesivir metaboliteGS443902GS 443902DNA/RNA SynthesisSARS-CoVRSVHCVDrug MetaboliteSARS coronavirusRespiratory syncytial virusHepatitis C virustriphosphatemetaboliteRemdesivirGS-5734RNA-dependentRNA-polymerasesRdRpTPGS-441524Inhibitorinhibitorinhibit

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