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[CAS NO. 1353625-73-6] Presatovir
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-16727 |
| Brand: | MCE |
| CAS: | 1353625-73-6 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 532.06 |
| Molecular Formula | C24H30ClN7O3S |
| SMILES | O=C(C(C=C(Cl)C=C1)=C1NS(C)(=O)=O)N(CCCC2)[C@@H]2C3=NN4C(N=C(N5CC[C@H](N)C5)C(C)=C4)=C3 |
3 Publications Citing Use of MCE
Summary
IC50 & Target
EC50: 0.43 nM (RSV) [1]
In Vitro
Presatovir is a novel, orally bioavailable RSV fusion inhibitor discovered following a lead optimization campaign on a hit originated from a phenotypic RSV antiviral high-throughput screen. Presatovir exhibits potent activity against a wide range of RSV A and B clinical isolates with a mean EC 50 value of 0.43 nM [1] . GS-5806 inhibits pre to post triggered conformational changes of RSV F protein, suggesting a possible mechanism for antiviral activity [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02254408 | Gilead Sciences |
Respiratory Syncytial Virus
|
January 23, 2015 | Phase 2 |
| NCT01801293 | Gilead Sciences |
RSV Infection
|
March 2013 | Phase 1 |
| NCT01797419 | Gilead Sciences |
Respiratory Syncytial Virus Infections
|
May 2013 | Phase 1 |
| NCT02254421 | Gilead Sciences |
Respiratory Syncytial Virus Infection
|
January 31, 2015 | Phase 2 |
| NCT02534350 | Gilead Sciences |
Respiratory Syncytial Virus (RSV)
|
December 31, 2015 | Phase 2 |
| NCT02135614 | Gilead Sciences |
Respiratory Syncytial Virus Infection
|
June 9, 2014 | Phase 2 |
| NCT01756482 | Gilead Sciences |
Respiratory Syncytial Virus Infections
|
November 2012 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 6 mg/mL ( 11.28 mM ; Need ultrasonic and warming)
H 2 O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.8795 mL | 9.3974 mL | 18.7949 mL |
| 5 mM | 0.3759 mL | 1.8795 mL | 3.7590 mL |
| 10 mM | 0.1879 mL | 0.9397 mL | 1.8795 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.6 mg/mL (1.13 mM); Clear solution
-
3.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 0.6 mg/mL (1.13 mM); Clear solution
-
4.
-
5.
Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)
Solubility: ≥ 0.48 mg/mL (0.90 mM); Clear solution
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.
- [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.
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