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| 5mg |
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| 10mg |
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| 50mg |
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Presatovir (GS-5806) is a novel and potent antiviral fusion inhibitor that is orally bioavailable and can inhibit RSV fusion protein with an EC50 value of 0.43 nM.
| ln Vitro |
Presatovir is a brand-new, orally accessible RSV fusion inhibitor that was found after a lead optimization effort on a hit that came from a high-throughput screen for phenotypic RSV antivirals. Against a variety of RSV A and B clinical isolates, presetovir demonstrates strong action, with an average EC50 value of 0.43 nM[1]. Pre-to post-triggered conformational changes of the RSV F protein are inhibited by GS-5806, indicating a potential mechanism of antiviral activity[2].
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| ln Vivo |
In a cotton rat model of RSV infection, prestatovir dose-dependent (0–30 mg/kg) exhibits antiviral effectiveness. Preclinical species exhibit oral bioavailability ranging from 46 to 100%, with Sprague-Dawley rats demonstrating the compound's entry into lung tissue. Presatovir oral therapy administered in many doses seems safe for adults, and in healthy human subjects experimentally infected with RSV, the high dose group shows a strong antiviral activity and a decrease in the severity of the disease. In order to inform future dose decisions, a PK-PD connection can be developed in a group receiving a lower dose of Presatovir[1].
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| References |
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| Additional Infomation |
Presatovir has been used in trials studying the treatment of RSV Infection, Respiratory Syncytial Virus (RSV), Respiratory Syncytial Virus Infections, and Respiratory Syncytial Virus (RSV) Infections.
Presatovir is an orally available inhibitor of human respiratory syncytial virus (RSV) fusion protein (F protein), with potential antiviral activity. Upon oral administration of GS-5806, this agent specifically binds to F protein on the viral surface, which inhibits RSV F protein-mediated fusion with the host cell membrane and prevents viral entry. This blocks RSV replication, reduces viral load, and decreases the severity of the disease. RSV F protein, a viral surface glycoprotein, plays a key role in RSV fusion with and entry into target cells. |
| Molecular Formula |
C24H30CLN7O3S
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|---|---|
| Molecular Weight |
532.06
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| Exact Mass |
531.181
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| CAS # |
1353625-73-6
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| PubChem CID |
58029842
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.735
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| LogP |
1.79
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
36
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| Complexity |
905
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC1=CN2C(=CC(=N2)[C@@H]3CCCCN3C(=O)C4=C(C=CC(=C4)Cl)NS(=O)(=O)C)N=C1N5CC[C@@H](C5)N
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| InChi Key |
GOFXWTVKPWJNGD-UWJYYQICSA-N
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| InChi Code |
InChI=1S/C24H30ClN7O3S/c1-15-13-32-22(27-23(15)30-10-8-17(26)14-30)12-20(28-32)21-5-3-4-9-31(21)24(33)18-11-16(25)6-7-19(18)29-36(2,34)35/h6-7,11-13,17,21,29H,3-5,8-10,14,26H2,1-2H3/t17-,21-/m0/s1
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| Chemical Name |
N-[2-[(2S)-2-[5-[(3S)-3-aminopyrrolidin-1-yl]-6-methylpyrazolo[1,5-a]pyrimidin-2-yl]piperidine-1-carbonyl]-4-chlorophenyl]methanesulfonamide
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| Synonyms |
GS-5806 GS 5806 GS5806
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~6 mg/mL (~11.28 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.6 mg/mL (1.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.6 mg/mL (1.13 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.6 mg/mL (1.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 0.48 mg/mL (0.90 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 0.48 mg/mL (0.90 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02135614 | COMPLETEDWITH RESULTS | Drug: Presatovir Drug: Presatovir placebo |
Respiratory Syncytial Virus Infection | Gilead Sciences | 2014-06-09 | Phase 2 |
| NCT02534350 | COMPLETEDWITH RESULTS | Drug: Presatovir Drug: Placebo |
Respiratory Syncytial Virus (RSV) | Gilead Sciences | 2015-12-31 | Phase 2 |
| NCT02254408 | COMPLETEDWITH RESULTS | Drug: Presatovir Drug: Placebo |
Respiratory Syncytial Virus | Gilead Sciences | 2015-01-23 | Phase 2 |
| NCT02254421 | COMPLETEDWITH RESULTS | Drug: Presatovir Drug: Placebo |
Respiratory Syncytial Virus Infection | Gilead Sciences | 2015-01-31 | Phase 2 |
| NCT01801293 | COMPLETED | Drug: GS-5806 | RSV Infection | Gilead Sciences | 2013-03 | Phase 1 |
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