Presatovir
Presatovir Basic information
- Product Name:
- Presatovir
- Synonyms:
-
- CS-2075
- Presatovir
- GS-5806
- N-(2-((S)-2-(5-((S)-3-aminopyrrolidin-1-yl)-6-methylpyrazolo[1,5-a]pyrimidin-2-yl)piperidine-1-carbonyl)-4-chlorophenyl)methanesulfonamide
- Presatovir (GS-5806)
- N-(2-{[(2S)-2-{5-[(3S)-3-Amino-1-pyrrolidinyl]-6-methylpyrazolo[1,5-a]pyrimidin-2-yl}-1-piperidinyl]carbonyl}-4-chlorophenyl)methanesulfonamide
- Methanesulfonamide, N-[2-[[(2S)-2-[5-[(3S)-3-amino-1-pyrrolidinyl]-6-methylpyrazolo[1,5-a]pyrimidin-2-yl]-1-piperidinyl]carbonyl]-4-chlorophenyl]-
- Presatovir,inhibit,Inhibitor,Respiratory syncytial virus,GS5806,GS 5806,RSV
- CAS:
- 1353625-73-6
- MF:
- C24H30ClN7O3S
- MW:
- 532.06
- Mol File:
- 1353625-73-6.mol
Presatovir Chemical Properties
- Density
- 1.54±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 6 mg/mL (11.28 mM);Water : < 0.1 mg/mL (insoluble)
- form
- Solid
- pka
- 7.12±0.10(Predicted)
- color
- Off-white to light yellow
- InChIKey
- GOFXWTVKPWJNGD-UWJYYQICSA-N
- SMILES
- CS(NC1=CC=C(Cl)C=C1C(N1CCCC[C@H]1C1C=C2N(N=1)C=C(C)C(N1CC[C@H](N)C1)=N2)=O)(=O)=O
Presatovir Usage And Synthesis
Uses
Presatovir (GS-5806) is an orally bioavailable RSV fusion inhibitor with a mean EC50 value of 0.43 nM[1].
in vivo
Presatovir demonstrates dose-dependent (0-30 mg/kg) antiviral efficacy in a cotton rat model of RSV infection. Oral bioavailability in preclinical species ranges from 46 to 100%, with penetration of the compound into the lung tissue demonstrated in Sprague-Dawley rats. Multidose oral treatment of Presatovir appears safe in adults, and in healthy human volunteers experimentally infected with RSV, a potent antiviral effect and reduction in disease severity is observed in the high dose group. A group treated with a lower dose of Presatovir allows for a PK-PD relationship to be established to help guide future dose selections[1].
References
[1] Mackman RL, et al. Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study. J Med Chem. 2015 Feb 26;58(4):1630-1643. DOI:10.1021/jm5017768
[2] Samuel D, et al. GS-5806 inhibits pre- to postfusion conformational changes of the respiratory syncytial virus fusion protein. Antimicrob Agents Chemother. 2015 Nov;59(11):7109-12. DOI:10.1128/AAC.00761-15
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