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Galidesivir (BCX4430 and Immucillin-A) is a novel adenosine analog and antiviral drug. Galidesivir was originally intended as a treatment for Hepatitis C, but subsequently developed as a potential treatment for deadly filovirus infections such as Ebola virus disease and Marburg virus disease. Galidesivir also shows broad-spectrum antiviral effectiveness against a range of other RNA virus families, including bunyaviruses, arenaviruses, paramyxoviruses, coronaviruses and flaviviruses. BCX4430 has been demonstrated to protect against both Ebola and Marburg viruses in both rodents and monkeys, even when administered up to 48 hours after infection.
| ln Vitro |
Gadesivir (BCX4430) is phosphorylated by cellular kinases to a triphosphate that resembles ATP; viral RNA polymerase incorporates the drug's monophosphate nucleotide into the RNA chain, resulting in an early termination of the chain [1]. Vero cell YFV infection is effectively inhibited by galidesivir. The neutral red absorption experiment yielded an EC50 of 8.3 μg/ml (24.5 μM) [3].
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| ln Vivo |
Galidesivir (BCX4430) is active in a range of experimental infections following intramuscular, intraperitoneal, and oral injection. Galidesivir has showed high efficacy in nonclinical studies involving fatal infections with Ebola, Marburg, Rift Valley disease, and yellow fever viruses [1]. Gardesivir (4 mg/kg; intraperitoneally; twice daily for 7 days) is efficacious in a hamster model of yellow fever (YF) [4].
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| Animal Protocol |
Animal/Disease Models: Female Syrian golden hamster (hamster infected with YF virus) [4]
Doses: 4 mg/kg body weight Route of Administration: intraperitoneal (ip) injection; twice a day for 7 days Experimental Results: Dramatically improved the survival of YFV-infected hamsters Rate. |
| References |
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| Additional Infomation |
Galidesivir is an adenosine analogue that has been investigated for use against Zaire Ebolavirus. In animal studies, galidesivir was effective in increasing the survival rates from infections caused by various pathogens, including Ebola, Marburg, Yellow Fever and Zika viruses. In vitro, it displayed broad-spectrum antiviral activity against various negative- and positive-sense RNA viruses, including coronaviruses, filoviruses, and arenaviruses. Phase 1 clinical trials have begun to determine the safety of this drug in humans. Because of its activity against other coronaviruses, it may be studied as a potential therapy for COVID-19.
Galidesivir is an adenosine analog and RNA polymerase inhibitor, with potential broad-spectrum antiviral activity. Upon administration, galidesivir is metabolized to its monophosphate form, which is then converted into the active triphosphate nucleotide. Galidesivir triphosphate binds to viral RNA-dependent RNA polymerase (RdRp) and gets incorporated into the growing viral RNA strand, which leads to premature chain termination. This prevents viral transcription and replication. Mechanism of Action Galidesivir works by binding to viral RNA polymerase where the natural nucleotide would bind, leading to the structural change in the viral enzyme due to altered electrostatic interactions. Disruption of viral RNA polymerase activity results in premature termination of the elongating RNA strand. Pharmacodynamics Galidesivir is an adenosine analogue with a broad-spectrum antiviral activity against RNA viruses, including flaviviruses, togaviruses, bunyaviruses, arenaviruses, paramyxoviruses, coronaviruses, filoviruses, orthomyxoviruses, and picornaviruses. |
| Molecular Formula |
C₁₁H₁₅N₅O₃
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|---|---|
| Molecular Weight |
265.27
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| Exact Mass |
265.117
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| CAS # |
249503-25-1
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| Related CAS # |
Galidesivir hydrochloride;222631-44-9
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| PubChem CID |
10445549
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
661.2±55.0 °C at 760 mmHg
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| Flash Point |
353.7±31.5 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.782
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| LogP |
-3.03
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
334
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1=C(C2=C(N1)C(=NC=N2)N)[C@H]3[C@@H]([C@@H]([C@H](N3)CO)O)O
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| InChi Key |
AMFDITJFBUXZQN-KUBHLMPHSA-N
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| InChi Code |
InChI=1S/C11H15N5O3/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)/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
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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 |
| 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) |
H2O : ~100 mg/mL (~376.97 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7697 mL | 18.8487 mL | 37.6974 mL | |
| 5 mM | 0.7539 mL | 3.7697 mL | 7.5395 mL | |
| 10 mM | 0.3770 mL | 1.8849 mL | 3.7697 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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