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Referencia número: HY-182761

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Antiviral agent 81

Antiviral agent 81 is an orally bioavailable N-acylated remdesivir derivative and RdRp inhibitor with 45.3% oral bioavailability (based on active metabolite GS-441524 exposure), plasma half-life >8 h, and reduced CYP3A4 inhibition. Antiviral agent 81 exhibits activity against Coronaviridae, Flaviviridae, and Pneumoviridae, and shows no activity against Orthomyxoviridae, Herpesviridae, and Alphaviridae. Antiviral agent 81 can be used for the research of viral infections.

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Fòrmula: C₃₂H₄₁N₆O₉P
Peso molecular:684.68

Almacenamiento:

Please store the product under the recommended conditions in the Certificate of Analysis.

Antiviral agent 81 Chemical Structure

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
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Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

RNA Polymerase

CYP1A2

CYP2C19

CYP2D6

CYP3A4

Ver todos los productos específicos de isoformas DNA/RNA Synthesis :

Ver todos los productos específicos de isoformas Cytochrome P450 :

In Vitro

Antiviral agent 81 (4f) potently inhibits SARS-CoV-2 in VeroE6-eGFP cells, with an EC₅₀ of 0.0862 μM, a CC₅₀ of 15.6 μM, and a selectivity index of 181.0^[1].
Antiviral agent 81 inhibits HCoV-OC43 (EC₅₀=0.90 μM) and HCoV-229E (EC₅₀=0.21 μM) in HEL299 cells, as well as YFV (EC₅₀=5.1 μM) and ZIKV (EC₅₀=4.1 μM) in U87 cells, with a CC₅₀ of 20.5 μM in U87 cells^[1].
Antiviral agent 81 (10 μM; 10 min) inhibits the CYP2C19, CYP2C9 and CYP3A4 subtypes in human liver microsomes, with the highest inhibition rate of 36.6% against CYP2C19, followed by 29.9% against CYP2C9 and 23.8% against CYP3A4^[1].
Antiviral agent 81 (100 μM; 0, 10, 30, 60, 120, 240 min) has an ex vivo plasma half-life of >8 h in human heparinized plasma, with a retention rate of approximately 70% after incubation at 37 °C for 4 h^[1].

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

Parmacokinetics

Species	Dose	Route	C_max	T_max	T_1/2	AUC_last	AUC_0-∞	MRT_last	MRT_0-∞	F
Rat^[1]	2 mg/kg	i.v.	95.2 ng/mL	0.5 h	1.6 h	248 ng·h/mL	269 ng·h/mL	2.11 h	2.60 h	/
Rat^[1]	10 mg/kg	p.o.	136 ng/mL	1.67 h	2.01 h	558 ng·h/mL	609 ng·h/mL	3.01 h	3.67 h	45.3 %

In Vivo

Antiviral agent 81 (4f) (2 mg/kg; tail vein injection; single dose; 24 h post-administration) is rapidly metabolized to the active metabolite GS-441524 (HY-103586) in male Sprague-Dawley rat models, with a C_maxof 95.2 ng/mL, a T_maxof 0.500 h, a T_1/2of 1.60 h, and an AUC_0-lastof 248 ng·h/mL^[1].
Antiviral agent 81 (10 mg/kg; p.o.; single dose; 24 h post-administration) is metabolized into the active metabolite GS-441524 in male Sprague-Dawley rat models, with a C_maxof 136 ng/mL, a T_maxof 1.67 h, a T_1/2of 2.01 h, an AUC_0-lastof 558 ng·h/mL, and an oral bioavailability of 45.3%^[1].

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

Chemical Information

Peso molecular 684.68
Fòrmula C₃₂H₄₁N₆O₉P
SMILES

O[C@@H]1[C@H](O)[C@@H](CO[P@@](N[C@@H](C)C(OCC(CC)CC)=O)(OC2=CC=CC=C2)=O)O[C@]1(C3=CC=C4C(NC(C5CCC5)=O)=NC=NN43)C#N
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Song L, et al. Discovery of orally bioavailable N-acylated remdesivir derivatives with potent broad-spectrum antiviral activity. Bioorg Chem. 2026;175:109758. [Content Brief]

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Concentration _(final) Concentration _(final)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Actividad biológica
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- In Vivo
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Antiviral agent 81

Ver todos los productos específicos de isoformas DNA/RNA Synthesis

Ver todos los productos específicos de isoformas Cytochrome P450

Actividad biológica

Chemical Information

Pureza y Documentación

Referencias

Calculators

Help & FAQs

Antiviral agent 81 Related Classifications

HY-182761 Related Classifications