| Size | Price | Stock | Qty |
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Purity: ≥98%
| Targets |
Galidesivir HCl targets viral RNA-dependent RNA polymerase (RdRp), an essential enzyme for the replication of RNA viruses. Upon cellular entry, galidesivir is metabolized to its monophosphate form and subsequently converted into the active triphosphate nucleotide. This active triphosphate metabolite binds to the viral RdRp with high affinity and is incorporated into the growing viral RNA strand. This incorporation leads to premature chain termination, effectively preventing viral transcription and replication. The compound exhibits tight binding to the SARS-CoV-2 RdRp, underlying its potential against emerging coronaviruses. As an adenosine analog, it mimics the natural substrate of the polymerase, allowing it to be efficiently recognized and incorporated by the viral enzyme.
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| ln Vitro |
Viral RNA polymerase incorporates the drug's monophosphate molecule into the expanding RNA chain, resulting in premature chain termination. Cell division phosphorylates Galidesivir (BCX4430) hydrochloride to a triphosphate that resembles ATP [1]. YFV infection of Vero cells is efficiently inhibited by hydrochloric acid. According to the neutral red food assay, the EC50 is 8.3 μg/mL (24.5 μM) [3].
Galidesivir HCl displays broad-spectrum in vitro antiviral activity against a wide range of RNA viruses from different families. It is active against filoviruses (Ebola, Marburg), coronaviruses including MERS-CoV, SARS-CoV, and SARS-CoV-2, as well as arenaviruses and flaviviruses. The compound's mechanism involves the inhibition of viral RdRp activity, with the active triphosphate form serving as a chain terminator during RNA synthesis. In cell-based assays, galidesivir effectively reduces viral replication across multiple RNA virus species at low micromolar concentrations. Its broad activity spectrum positions it as a promising candidate for treating emerging viral diseases and pandemic threats. |
| ln Vivo |
Hydrochloride galidesivir (BCX4430) administered intramuscularly, intraperitoneally, orally, is effective against a range of experimental infections. In nonclinical tests including deadly infections with the Ebola, Marburg, Rift Valley disease, and yellow fever viruses, galidevir hydrochloride has demonstrated a notable level of efficacy [1]. In a hamster model of yellow fever (YF), galidevir hydrochloride (4 mg/kg; intraperitoneal injection; twice daily for 7 days) is efficacious [4].
In vivo, galidesivir hydrochloride has demonstrated significant efficacy in increasing survival rates in animal models infected with various high-consequence pathogens. It has shown protective effects against Ebola virus, Marburg virus, Yellow Fever virus, and Zika virus infections in preclinical studies. The compound's in vivo efficacy is attributed to its ability to achieve therapeutic concentrations in target tissues and effectively inhibit viral replication through RdRp inhibition. Its activity against multiple coronaviruses in vitro suggests potential for in vivo evaluation against COVID-19 and related diseases. The compound has progressed to Phase 1 clinical trials to evaluate its safety and pharmacokinetic profile in humans. |
| Enzyme Assay |
In vitro enzyme assays for Galidesivir HCl typically involve measuring the inhibition of viral RNA-dependent RNA polymerase activity using purified enzyme preparations and synthetic RNA templates. The active triphosphate metabolite is tested for its ability to compete with natural nucleotide substrates and incorporate into nascent RNA strands, causing chain termination. Binding affinity to RdRp is assessed using biochemical techniques such as surface plasmon resonance or fluorescence polarization. Enzyme kinetic studies determine the mechanism of inhibition and the potency of the compound against various viral polymerases. These cell-free assays provide critical information on the compound's direct antiviral mechanism and its specificity for viral versus host polymerases.
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| Cell Assay |
In vitro cell-based assays for Galidesivir HCl involve treating virus-infected cell cultures with varying concentrations of the compound to assess its antiviral efficacy. Common cell lines used include Vero cells, HEK-293 cells, and other permissive cell lines for specific viruses. Cells are infected with the virus of interest (e.g., Ebola, SARS-CoV-2, Zika) and then treated with galidesivir at multiple concentrations. Viral replication is quantified by measuring viral RNA levels via RT-qPCR, plaque reduction assays, or by assessing cytopathic effect reduction. The half-maximal effective concentration (EC50) is determined from dose-response curves. Cytotoxicity is simultaneously assessed to calculate the selectivity index.
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| Animal Protocol |
Animal/Disease Models: Female Syrian golden hamsters (hamsters infected with YF virus)[4]
Doses: 4 mg/kg of body weight Route of Administration: Ip; twice a day for 7 days Experimental Results: Dramatically improved the survival rate of hamsters infected with YFV . In vivo animal experiments for Galidesivir HCl have been conducted in rodent and non-human primate models infected with various RNA viruses. Animal models include mice and guinea pigs infected with Ebola virus, Marburg virus, Yellow Fever virus, and Zika virus. The compound is typically administered via intraperitoneal or intramuscular injection, with dosing schedules optimized for each pathogen. Survival rates, viral load reduction in tissues, and clinical signs of disease are monitored as primary efficacy endpoints. Pharmacokinetic-pharmacodynamic relationships are established to guide dose selection. These studies have demonstrated significant improvements in survival and reduction in viral burden. |
| ADME/Pharmacokinetics |
Galidesivir HCl is characterized by favorable pharmacokinetic properties including good aqueous solubility (41 mg/mL in water). Following administration, the compound is rapidly converted intracellularly to its active triphosphate form, which persists at therapeutic levels. The hydrochloride salt formulation enhances solubility and bioavailability compared to the free base. The compound is typically administered via injection in preclinical studies, with good distribution to target tissues. Formulation for in vivo studies can be prepared using water or isotonic buffers. Pharmacokinetic parameters such as half-life, volume of distribution, and clearance have been characterized in animal models, supporting its progression to clinical trials.
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| Toxicity/Toxicokinetics |
Available toxicity data for Galidesivir HCl is limited to preclinical studies and early-phase clinical trials. The compound has been evaluated in animal models for safety pharmacology and toxicology as part of its development for filovirus infections. Standard toxicological assessments include acute and repeated-dose toxicity studies in rodents and non-human primates. The compound is generally well-tolerated at therapeutic doses, with a safety margin sufficient to support clinical development. As with other nucleoside analogs, potential off-target effects on host polymerases are carefully monitored. Phase 1 clinical trials are designed to establish the safety and tolerability profile in humans.
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| References |
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| Additional Infomation |
Galidisevir hydrochloride is the hydrochloride form of galidisevir, an adenosine analog and RNA polymerase inhibitor with potential broad-spectrum antiviral activity. After administration, galidisevir is metabolized to a monophosphate form, which is then converted to the active triphosphate. The galidisevir triphosphate binds to viral RNA-dependent RNA polymerase (RdRp) and is incorporated into the elongating viral RNA chain, causing premature chain termination. This prevents viral transcription and replication.
See also: Galidisevir (note moved to). Galidesivir HCl is a direct-acting antiviral agent with broad-spectrum activity against RNA viruses. It functions as an adenosine analog that, upon intracellular phosphorylation to its active triphosphate form, inhibits viral RNA-dependent RNA polymerase through chain termination. The compound was originally developed for Hepatitis C and later repurposed for filovirus infections, demonstrating significant in vivo efficacy against Ebola, Marburg, Yellow Fever, and Zika viruses. Its activity against multiple coronaviruses, including SARS-CoV-2, has prompted investigation as a potential COVID-19 therapeutic. Galidesivir HCl has entered Phase 1 clinical trials for safety evaluation. The compound is also known by the synonyms Immucillin-A hydrochloride and BCX 4430 hydrochloride. |
| Molecular Formula |
C11H15N5O3.HCL
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|---|---|
| Molecular Weight |
301.72944
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| Exact Mass |
301.094
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| CAS # |
222631-44-9
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| Related CAS # |
Galidesivir;249503-25-1
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| PubChem CID |
69211190
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
334
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O[C@H]1[C@H](C2=CNC3=C2N=CN=C3N)N[C@H](CO)[C@H]1O.Cl
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| InChi Key |
PCCHVYNGFMEGIG-QPAIBFMUSA-N
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| InChi Code |
InChI=1S/C11H15N5O3.ClH/c12-11-8-6(14-3-15-11)4(1-13-8)7-10(19)9(18)5(2-17)16-7/h1,3,5,7,9-10,13,16-19H,2H2,(H2,12,14,15)1H/t5-,7+,9-,10+/m1./s1
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| Chemical Name |
(2S,3S,4R,5R)-2-(4-amino-5H-pyrrolo[3,2-d]pyrimidin-7-yl)-5-(hydroxymethyl)pyrrolidine-3,4-diol hydrochloride
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| Synonyms |
BCX4430 BCX 4430 BCX-4430. Immucillin-A.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~105 mg/mL (~347.99 mM)
H2O : ≥ 41 mg/mL (~135.88 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5.25 mg/mL (17.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 52.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5.25 mg/mL (17.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 52.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 100 mg/mL (331.42 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.3314 mL | 1.6571 mL | 3.3142 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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