ALS-8176 (active form) Chemical Properties

Boiling point:

532.8±60.0 °C(Predicted)

Density 

1.78±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO : ≥ 47 mg/mL (160.04 mM)

form 

Solid

pka

12.47±0.70(Predicted)

color 

White to off-white

ALS-8176 (active form) Usage And Synthesis

Uses

ALS-8112 is a potent and selective respiratory syncytial virus (RSV) polymerase inhibitor. The 5'-triphosphate form of ALS-8112 inhibits RSV polymerase with an IC50 of 0.02 μM.

References

[1] Wang G, et al. Discovery of 4'-chloromethyl-2'-deoxy-3',5'-di-O-isobutyryl-2'-fluorocytidine (ALS-8176), a first-in-class RSV polymerase inhibitor for treatment of human respiratory syncytial virus infection. J Med Chem. 2015 Feb 26;58(4):1862-78. DOI:10.1021/jm5017279
[2] Jordan PC, et al. Activation Pathway of a Nucleoside Analog Inhibiting Respiratory Syncytial Virus Polymerase. ACS Chem Biol. 2017 Jan 20;12(1):83-91. DOI:10.1021/acschembio.6b00788
[3] DeVincenzo JP, et al. Activity of Oral ALS-008176 in a Respiratory Syncytial Virus Challenge Study. N Engl J Med. 2015 Nov 19;373(21):2048-58. DOI:10.1056/NEJMoa1413275
[4] Deval J, et al. Molecular Basis for the Selective Inhibition of Respiratory Syncytial Virus RNA Polymerase by 2'-Fluoro-4'-Chloromethyl-Cytidine Triphosphate. PLoS Pathog. 2015 Jun 22;11(6):e1004995. DOI:10.1371/journal.ppat.1004995