| Identification | Back Directory | [Name]
3,4-Pyrrolidinediol, 2-(4-amino-5H-pyrrolo3,2-dpyrimidin-7-yl)-5-(hydroxymethyl)-, (2S,3S,4R,5R)- | [CAS]
249503-25-1 | [Synonyms]
Immucillin-A
BCX4430 (freebase)
GALIDESIVIR (BCX 4430)
BCX4430 freebase
(Galidesivir)
(2S,3S,4R,5R)-2-(4-AMINO-5H-PYRROLO[3,2-D]PYRIMIDIN-7-YL)-5-(HYDROXYMETHYL)PYRROLIDINE-3,4-DIOL
3,4-Pyrrolidinediol, 2-(4-amino-5H-pyrrolo3,2-dpyrimidin-7-yl)-5-(hydroxymethyl)-, (2S,3S,4R,5R)- | [Molecular Formula]
C11H15N5O3 | [MDL Number]
MFCD28385877 | [MOL File]
249503-25-1.mol | [Molecular Weight]
265.27 |
| Chemical Properties | Back Directory | [Boiling point ]
661.2±55.0 °C(Predicted) | [density ]
1.630±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
13.78±0.40(Predicted) | [color ]
White to off-white | [Water Solubility ]
Water : 1.53 mg/mL (5.77 mM) |
| Hazard Information | Back Directory | [Uses]
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[1][2][3]. | [in vivo]
Galidesivir (BCX4430) 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 has demonstrated pronounced efficacy[1].
Galidesivir (4 mg/kg; i.p.; twice daily for 7 days) is effectively in a hamster model of yellow fever (YF)[4]. | 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.
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| [References]
[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. DOI:10.1016/j.jiph.2016.04.002
[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. DOI:10.1016/j.lfs.2020.117592
[3] Warren TK, et al. Protection against filovirus diseases by a novel broad-spectrum nucleoside analogue BCX4430. Nature. 2014;508(7496):402-405. DOI:10.1038/nature13027
[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. DOI:10.1128/AAC.03368-14 |
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Musechem
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