| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| Other Sizes |
Purity: ≥98%
| Targets |
RV521 targets the RSV fusion (F) protein, which is essential for viral entry into host cells. The F protein mediates fusion of the viral envelope with the host cell membrane, allowing the viral genome to enter the cell. By inhibiting the F protein, RV521 blocks viral entry and prevents infection. The compound has IC50 values of 1.4 nM for RSV-A and 1.0 nM for RSV-B.
|
|---|---|
| ln Vitro |
Kinase Assay: Cell Assay: In vitro, RV521 demonstrates potent efficacy against a panel of clinical isolates of RSV-A and RSV-B viruses, with IC50s of 1.4 nM and 1.0 nM, respectively. The compound shows promising pharmaceutical properties, including potent antiviral activity. Specific cellular assay data, such as EC50 values for inhibition of viral replication in cell lines, are not detailed in the available sources beyond its characterization as a highly potent RSV F protein inhibitor. |
| ln Vivo |
RV521 has been evaluated in preclinical and clinical studies for the treatment of RSV disease. As an orally bioactive compound, it offers the potential for convenient oral administration in therapeutic applications. The compound is currently in clinical development for the treatment of RSV disease in vulnerable patient populations. Specific animal model data are not detailed in the available sources. |
| Enzyme Assay |
The RSV fusion protein inhibition assay for RV521 involves incubating the compound with RSV F protein and a fluorescently labeled peptide substrate that mimics the host cell membrane. The fusion activity of the F protein is measured by the change in fluorescence upon membrane fusion. IC50 values are calculated from dose-response curves. Alternatively, a cell-based fusion assay can be performed using cells expressing RSV F protein and target cells loaded with a fluorescent dye.
|
| Cell Assay |
To evaluate the antiviral activity of RV521, RSV-susceptible cell lines (such as HEp-2 or A549 cells) are seeded in 96-well plates and infected with RSV (RSV-A or RSV-B strains) in the presence of varying concentrations of RV521. After 48-72 hours of incubation, viral replication is assessed by measuring the cytopathic effect (CPE) or by quantifying viral RNA using RT-PCR. The EC50 for inhibition of viral replication is calculated. Cell viability is monitored to ensure that observed antiviral effects are not due to cytotoxicity.
|
| Animal Protocol |
The in vivo efficacy of RV521 is evaluated in mouse models of RSV infection. Immunocompetent or immunodeficient mice are infected intranasally with RSV. After infection, mice are treated with RV521 orally at various doses, typically administered once or twice daily. At the end of the treatment period (e.g., 3-5 days post-infection), animals are euthanized, and lung tissue is collected. Viral titers in lung homogenates are determined by plaque assay or by quantifying viral RNA using RT-PCR. The reduction in viral titer is expressed as the log10 reduction compared to vehicle-treated controls.
|
| ADME/Pharmacokinetics |
RV521 is characterized as being orally bioactive. Specific pharmacokinetic parameters (e.g., Cmax, Tmax, half-life, AUC) are not detailed in the available sources. The compound has a molecular weight of 446.44 and a molecular formula of C23H22F4N4O. It is soluble in DMSO at 3.33 mg/mL. It is typically stored at -20°C for long-term stability.
|
| Toxicity/Toxicokinetics |
Specific toxicity data for RV521 are not provided in the available sources. As a compound that has advanced to clinical development, its safety profile has been assessed in preclinical toxicology studies and early-phase clinical trials. The compound is intended for the treatment of RSV disease and is not approved for general use. Standard safety precautions should be followed when handling this compound.
|
| References | |
| Additional Infomation |
Sisunatovir is being investigated in the clinical trial NCT04267822 (RV521 study of adult patients with upper respiratory tract infections complicated by respiratory syncytial virus infection following hematopoietic stem cell transplantation). Sisunatovir is an oral small molecule inhibitor that inhibits the human respiratory syncytial virus (RSV) fusion protein (F protein) and has potential antiviral activity. After oral administration, sisunatovir specifically targets and binds to the RSV-F protein on the viral surface, thereby inhibiting RSV-F protein-mediated viral fusion with the host cell membrane and preventing viral entry into the cell. This can block RSV replication, reduce viral load, and alleviate disease severity. The RSV-F protein is a viral surface glycoprotein that plays a crucial role in RSV fusion with and entry into target cells.
RV521 is also known as Sisunatovir. It is an orally bioactive, highly potent small-molecule inhibitor of RSV fusion protein with IC50s of 1.4 nM for RSV-A and 1.0 nM for RSV-B. It is currently in clinical development for the treatment of RSV disease in pediatrics, the elderly, and immune-compromised patients. |
| Molecular Formula |
C23H22F4N4O
|
|
|---|---|---|
| Molecular Weight |
446.440598964691
|
|
| Exact Mass |
446.172
|
|
| CAS # |
1903763-82-5
|
|
| Related CAS # |
Sisunatovir hydrochloride;1903763-83-6
|
|
| PubChem CID |
132016492
|
|
| Appearance |
White to off-white solid powder
|
|
| LogP |
3.1
|
|
| Hydrogen Bond Donor Count |
1
|
|
| Hydrogen Bond Acceptor Count |
7
|
|
| Rotatable Bond Count |
6
|
|
| Heavy Atom Count |
32
|
|
| Complexity |
715
|
|
| Defined Atom Stereocenter Count |
0
|
|
| SMILES |
FC1C=CC2=C(C=1)N(CC1=NC3C=C(CN)C=CC=3N1CCCC(F)(F)F)C(C12CC1)=O
|
|
| InChi Key |
JOPCJJSYRPUEDS-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C23H22F4N4O/c24-15-3-4-16-19(11-15)31(21(32)22(16)7-8-22)13-20-29-17-10-14(12-28)2-5-18(17)30(20)9-1-6-23(25,26)27/h2-5,10-11H,1,6-9,12-13,28H2
|
|
| Chemical Name |
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| 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)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.60 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 25.0 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: ≥ 2.5 mg/mL (5.60 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 25.0 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: ≥ 2.5 mg/mL (5.60 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2399 mL | 11.1997 mL | 22.3994 mL | |
| 5 mM | 0.4480 mL | 2.2399 mL | 4.4799 mL | |
| 10 mM | 0.2240 mL | 1.1200 mL | 2.2399 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA