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

GS-443902 (Synonyms: 瑞德西韦代谢物; GS-441524 triphosphate; Remdesivir metabolite)

目录号: HY-126303 纯度: 99.87%
产品使用指南

GS-443902 (GS-441524 triphosphate) 是一种有效的病毒 RNA 依赖的 RNA 聚合酶 (RdRp) 抑制剂,对 RSV RdRp 和 HCV RdRp 的 IC50 分别为 1.1 µM 和 5 µM。GS-443902 是 Remdesivir 的活性三磷酸盐代谢产物。

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GS-443902 Chemical Structure

GS-443902 Chemical Structure

CAS No. : 1355149-45-9

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Description

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]

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 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].

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 t1/2 of 14 h and levels required for >50% virus inhibition for 24 hours[3].

Molecular Weight

531.20

Formula

C₁₂H₁₆N₅O₁₃P₃

CAS No.

1355149-45-9

中文名称

瑞德西韦代谢物

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 argon

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under argon)

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
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under argon)。 -80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

References

Purity: 99.87%

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The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

GS-443902GS-441524 triphosphateRemdesivir metaboliteGS443902GS 443902DNA/RNA SynthesisSARS-CoVRSVHCVDrug MetaboliteSARS coronavirusRespiratory syncytial virusHepatitis C virustriphosphatemetaboliteRemdesivirGS-5734RNA-dependentRNA-polymerasesRdRpTPGS-441524Inhibitorinhibitorinhibit

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GS-443902
目录号:
HY-126303
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