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> Galidesivir (hydrochloride) [222631-44-9]

Galidesivir (hydrochloride) [222631-44-9]

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Galidesivir (BCX4430) hydrochloride, an adenosine analog and a direct-acting antiviral agent, disrupts viral RNA-dependent RNA polymerase (RdRp) activity. Galidesivir hydrochloride 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 hydrochloride inhibits some negative-sense RNA viruses with EC50s ranging from ~3 to ~68 μM.

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Galidesivir hydrochloride Chemical Structure

Galidesivir hydrochloride Chemical Structure

CAS No. : 222631-44-9

This product is a controlled substance and not for sale in your territory.

Based on 8 publication(s) in Google Scholar

Other Forms of Galidesivir hydrochloride:

  • Galidesivir In-stock
  • Galidesivir dihydrochloride Obtenir un devis

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Description

Galidesivir (BCX4430) hydrochloride, an adenosine analog and a direct-acting antiviral agent, disrupts viral RNA-dependent RNA polymerase (RdRp) activity. Galidesivir hydrochloride 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 hydrochloride inhibits some negative-sense RNA viruses with EC50s ranging from ~3 to ~68 μM[1][2][3].

IC50 & Target

RdRp inhibitor
In Vitro

Cellular kinases phosphorylate Galidesivir (BCX4430) hydrochloride to a triphosphate that mimics ATP; viral RNA polymerases incorporate the drug's monophosphate nucleotide into the growing RNA chain, causing premature chain termination[1].
Galidesivir hydrochloride effectively inhibits the infection of Vero cells with YFV. The EC50 determined by the neutral red uptake assay is 8.3 μg/ml (24.5 μM)[3].

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

Galidesivir hydrochloride Related Antibodies
In Vivo

Galidesivir (BCX4430) hydrochloride is active after intramuscular, intraperitoneal, and oral administration in a variety of experimental infections. In nonclinical studies involving lethal infections with Ebola virus, Marburg virus, Rift Valley fever virus, and Yellow Fever virus, Galidesivir hydrochloride has demonstrated pronounced efficacy[1].
Galidesivir hydrochloride (4 mg/kg; i.p.; twice daily for 7 days) is effectively in a hamster model of yellow fever (YF)[4].

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

Animal Model: Female Syrian golden hamsters (hamsters infected with YF virus)[4]
Dosage: 4 mg/kg of body weight
Administration: I.p.; twice daily for 7 days
Result: Significantly improved the survival of hamsters infected with YFV.
Essai clinique
Masse moléculaire

301.73

Formule

C11H16ClN5O3
CAS No.

222631-44-9
Appearance

Solid

Color

White to yellow

SMILES

O[C@H]1[C@H](C2=CNC3=C2N=CN=C3N)N[C@H](CO)[C@H]1O.Cl
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvant et solubilité
In Vitro: 

DMSO : 105 mg/mL (347.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 41 mg/mL (135.88 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3142 mL 16.5711 mL 33.1422 mL
5 mM 0.6628 mL 3.3142 mL 6.6284 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* 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.

  • Calculateur de molarité

  • Calculateur de dilution

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5.25 mg/mL (17.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 5.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (52.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5.25 mg/mL (17.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 5.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (52.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (331.42 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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).
Pureté et documentation

Purity: 99.89%

COA (255 KB) LCMS (108 KB)

Instruction de manipulation (2659 KB)
Références

  • [1]. Taylor R, et al. BCX4430 - A broad-spectrum antiviral adenosine nucleoside analog under development for the treatment of Ebola virus disease. J Infect Public Health. 2016;9(3):220-226.  [Content Brief]

    [2]. Elfiky AA, et al. ICN-1229, Remdesivir, PSI-7977, Galidesivir, and GS 1278 against SARS-CoV-2 RNA dependent RNA polymerase (RdRp): A molecular docking study. Life Sci. 2020 Mar 25:117592.  [Content Brief]

    [3]. Warren TK, et al. Protection against filovirus diseases by a novel broad-spectrum nucleoside analogue BCX4430. Nature. 2014;508(7496):402-405.  [Content Brief]

    [4]. Julander JG, et al. BCX4430, a novel nucleoside analog, effectively treats yellow fever in a Hamster model. Antimicrob Agents Chemother. 2014;58(11):6607-6614.  [Content Brief]

  • [1]. Taylor R, et al. BCX4430 - A broad-spectrum antiviral adenosine nucleoside analog under development for the treatment of Ebola virus disease. J Infect Public Health. 2016;9(3):220-226.

    [2]. Elfiky AA, et al. ICN-1229, Remdesivir, PSI-7977, Galidesivir, and GS 1278 against SARS-CoV-2 RNA dependent RNA polymerase (RdRp): A molecular docking study. Life Sci. 2020 Mar 25:117592.

    [3]. Warren TK, et al. Protection against filovirus diseases by a novel broad-spectrum nucleoside analogue BCX4430. Nature. 2014;508(7496):402-405.

    [4]. Julander JG, et al. BCX4430, a novel nucleoside analog, effectively treats yellow fever in a Hamster model. Antimicrob Agents Chemother. 2014;58(11):6607-6614.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.3142 mL 16.5711 mL 33.1422 mL 82.8555 mL
5 mM 0.6628 mL 3.3142 mL 6.6284 mL 16.5711 mL
10 mM 0.3314 mL 1.6571 mL 3.3142 mL 8.2856 mL
15 mM 0.2209 mL 1.1047 mL 2.2095 mL 5.5237 mL
20 mM 0.1657 mL 0.8286 mL 1.6571 mL 4.1428 mL
25 mM 0.1326 mL 0.6628 mL 1.3257 mL 3.3142 mL
30 mM 0.1105 mL 0.5524 mL 1.1047 mL 2.7619 mL
40 mM 0.0829 mL 0.4143 mL 0.8286 mL 2.0714 mL
50 mM 0.0663 mL 0.3314 mL 0.6628 mL 1.6571 mL
60 mM 0.0552 mL 0.2762 mL 0.5524 mL 1.3809 mL
80 mM 0.0414 mL 0.2071 mL 0.4143 mL 1.0357 mL
100 mM 0.0331 mL 0.1657 mL 0.3314 mL 0.8286 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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Galidesivir hydrochloride Related Classifications

  • Cell Cycle/DNA Damage Anti-infection
  • DNA/RNA Synthesis SARS-CoV Filovirus
Help & FAQs

Keywords:

Galidesivir222631-44-9BCX4430Immucillin-ABCX 4430BCX-4430DNA/RNA SynthesisSARS-CoVFilovirusSARS coronavirusadenosinenucleosideanalogvirusinfectionpathogenicCOVID-19Inhibitorinhibitorinhibit

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