| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| Other Sizes |
Purity: ≥98%
| Targets |
RV521 HCl 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. By inhibiting the F protein, RV521 HCl blocks viral entry and prevents infection. The active free base 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 HCl demonstrates potent antiviral activity against RSV, consistent with the active free base RV521. The compound shows 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 HCl salt form is designed to improve the pharmaceutical properties of the compound for formulation and administration. |
| ln Vivo |
RV521 HCl 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. 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 HCl involves incubating the compound with RSV F protein and a fluorescently labeled peptide substrate. 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. As the HCl salt is expected to have the same activity as the free base, the assay is performed using the active compound.
|
| Cell Assay |
To evaluate the antiviral activity of RV521 HCl, RSV-susceptible cell lines (such as HEp-2 or A549 cells) are seeded in 96-well plates and infected with RSV in the presence of varying concentrations of RV521 HCl. 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 using an MTT or CellTiter-Glo assay.
|
| Animal Protocol |
The in vivo efficacy of RV521 HCl is evaluated in mouse models of RSV infection. Immunocompetent or immunodeficient mice are infected intranasally with RSV. After infection, mice are treated with RV521 HCl orally at various doses. At the end of the treatment period, 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 HCl is characterized as being orally bioactive. The HCl salt form is designed to enhance solubility and stability for pharmaceutical formulation. Specific pharmacokinetic parameters (e.g., Cmax, Tmax, half-life, AUC) are not detailed in the available sources. The compound is typically stored at -20°C for long-term stability.
|
| Toxicity/Toxicokinetics |
Specific toxicity data for RV521 HCl 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 hydrochloride is the hydrochloride form of Sisunatovir, an orally administered small molecule inhibitor that inhibits the human respiratory syncytial virus (RSV) fusion protein (F protein), exhibiting 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 the fusion of RSV with target cells and their entry into the target cell.
RV521 HCl is the hydrochloride salt of RV521 (Sisunatovir). It is an orally bioactive, highly potent small-molecule inhibitor of RSV fusion protein. The active free base has 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. |
| Molecular Formula |
C23H23CLF4N4O
|
|
|---|---|---|
| Molecular Weight |
482.901538133621
|
|
| Exact Mass |
482.149
|
|
| Elemental Analysis |
C, 57.21; H, 4.80; Cl, 7.34; F, 15.74; N, 11.60; O, 3.31
|
|
| CAS # |
1903763-83-6
|
|
| Related CAS # |
Sisunatovir;1903763-82-5
|
|
| PubChem CID |
153520065
|
|
| Appearance |
Off-white to light yellow solid powder
|
|
| Hydrogen Bond Donor Count |
2
|
|
| Hydrogen Bond Acceptor Count |
7
|
|
| Rotatable Bond Count |
6
|
|
| Heavy Atom Count |
33
|
|
| Complexity |
715
|
|
| Defined Atom Stereocenter Count |
0
|
|
| InChi Key |
NYYYAFKAHRIPJW-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C23H22F4N4O.ClH/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;1H
|
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
|
| 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 (5.18 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 (5.18 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 (5.18 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 | 2.0708 mL | 10.3541 mL | 20.7082 mL | |
| 5 mM | 0.4142 mL | 2.0708 mL | 4.1416 mL | |
| 10 mM | 0.2071 mL | 1.0354 mL | 2.0708 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