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ChemicalBook >  Product Catalog >  Biochemical Engineering >  Biochemical Reagents >  Agonist Inhibitors >  3,4-Pyrrolidinediol, 2-(4-amino-5H-pyrrolo3,2-dpyrimidin-7-yl)-5-(hydroxymethyl)-, (2S,3S,4R,5R)-

3,4-Pyrrolidinediol, 2-(4-amino-5H-pyrrolo3,2-dpyrimidin-7-yl)-5-(hydroxymethyl)-, (2S,3S,4R,5R)-

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3,4-Pyrrolidinediol, 2-(4-amino-5H-pyrrolo3,2-dpyrimidin-7-yl)-5-(hydroxymethyl)-, (2S,3S,4R,5R)- Basic information

Product Name:
3,4-Pyrrolidinediol, 2-(4-amino-5H-pyrrolo3,2-dpyrimidin-7-yl)-5-(hydroxymethyl)-, (2S,3S,4R,5R)-
Synonyms:
  • 3,4-Pyrrolidinediol, 2-(4-amino-5H-pyrrolo3,2-dpyrimidin-7-yl)-5-(hydroxymethyl)-, (2S,3S,4R,5R)-
  • BCX4430 (freebase)
  • (2S,3S,4R,5R)-2-(4-AMINO-5H-PYRROLO[3,2-D]PYRIMIDIN-7-YL)-5-(HYDROXYMETHYL)PYRROLIDINE-3,4-DIOL
  • BCX4430 freebase (Galidesivir)
  • GALIDESIVIR (BCX 4430)
  • Immucillin-A
CAS:
249503-25-1
MF:
C11H15N5O3
MW:
265.27
Mol File:
249503-25-1.mol
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3,4-Pyrrolidinediol, 2-(4-amino-5H-pyrrolo3,2-dpyrimidin-7-yl)-5-(hydroxymethyl)-, (2S,3S,4R,5R)- Chemical Properties

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)
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3,4-Pyrrolidinediol, 2-(4-amino-5H-pyrrolo3,2-dpyrimidin-7-yl)-5-(hydroxymethyl)-, (2S,3S,4R,5R)- Usage And Synthesis

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.

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

3,4-Pyrrolidinediol, 2-(4-amino-5H-pyrrolo3,2-dpyrimidin-7-yl)-5-(hydroxymethyl)-, (2S,3S,4R,5R)-Supplier

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