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Galidesivir

Cat. No. M29677
Galidesivir Structure
Synonym:

BCX4430; Immucillin-A

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Biological Activity

Galidesivir (BCX4430), an adenosine analog and a direct-acting antiviral agent, disrupts viral RNA-dependent RNA polymerase (RdRp) activity. Galidesivir is active in vitro against many RNA viral pathogens, including the filoviruses and emerging infectious agents such as MERS-CoV, SARS-CoV, and SARS-CoV-2. Galidesivir inhibits some negative-sense RNA viruses with EC50s ranging from ~3 to ~68 μM.

Chemical Information
Molecular Weight 265.27
Formula C11H15N5O3
CAS Number 249503-25-1
Form Solid
Solubility (25°C) Water 1.53 mg/mL (Need ultrasonic and warming)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Amanda Mathis, et al. Clin Pharmacol Drug Dev. Pharmacokinetics and Safety of the Nucleoside Analog Antiviral Drug Galidesivir Administered to Healthy Adult Subjects

[2] Ray Taylor, et al. Viruses. Activity of Galidesivir in a Hamster Model of SARS-CoV-2

[3] Justin G Julander, et al. Antiviral Res. An update on the progress of galidesivir (BCX4430), a broad-spectrum antiviral

[4] Jonna B Westover, et al. Antiviral Res. Galidesivir limits Rift Valley fever virus infection and disease in Syrian golden hamsters

[5] Kevin J Sparrow, et al. ACS Med Chem Lett. An Isomer of Galidesivir That Potently Inhibits Influenza Viruses and Members of the Bunyavirales Order

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Keywords: Galidesivir, BCX4430; Immucillin-A supplier, DNA/RNA Synthesis, inhibitors, activators


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