| Identification | Back Directory | [Name]
Presatovir | [CAS]
1353625-73-6 | [Synonyms]
CS-2075
GS-5806
Presatovir
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
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]- | [Molecular Formula]
C24H30ClN7O3S | [MDL Number]
MFCD28963961 | [MOL File]
1353625-73-6.mol | [Molecular Weight]
532.06 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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]. | [storage]
Store at -20°C | [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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| Company Name: |
DKMbiochem.Co. Ltd Gold
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| Telephone: |
15901859516 |
| Website: |
http://www.dkmbiochem.com/ |
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