MedKoo Cat#: 571523 | Name: Sisunatovir free base
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Sisunatovir, also known as RV521, is a highly potent fusion inhibitor with efficacy against a panel of clinical isolates of RSV-A and RSV-B viruses. RV521 exhibited a mean IC50 of 1.2 nM against a panel of RSV A and B laboratory strains and clinical isolates with antiviral efficacy in the Balb/C mouse model of RSV infection. Oral bioavailability in preclinical species ranged from 42 to >100% with evidence of highly efficient penetration into lung tissue. In healthy adult human volunteers experimentally infected with RSV, a potent antiviral effect was observed with a significant reduction in viral load and symptoms compared to placebo.

Chemical Structure

Sisunatovir free base
CAS#1903763-82-5 (free base)

Theoretical Analysis

MedKoo Cat#: 571523

Name: Sisunatovir free base

CAS#: 1903763-82-5 (free base)

Chemical Formula: C23H22F4N4O

Exact Mass: 446.1730

Molecular Weight: 446.45

Elemental Analysis: C, 61.88; H, 4.97; F, 17.02; N, 12.55; O, 3.58

Price and Availability

Size Price Availability Quantity
5mg USD 450.00 2 Weeks
10mg USD 700.00 2 Weeks
50mg USD 1,750.00 2 Weeks
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Synonym
RV521; RV-521; RV 521; Sisunatovir;
IUPAC/Chemical Name
1'-((5-(aminomethyl)-1-(4,4,4-trifluorobutyl)-1H-benzo[d]imidazol-2-yl)methyl)-6'-fluorospiro[cyclopropane-1,3'-indolin]-2'-one
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
SMILES Code
O=C1C2(CC2)C3=C(C=C(F)C=C3)N1CC4=NC5=C(N4CCCC(F)(F)F)C=CC(CN)=C5
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Biological target:
Sisunatovir is a RSV protein inhibitor that exhibits 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.
In vitro activity:
To be determined
In vivo activity:
After infection with RSV in healthy volunteers and treatment with Sisunatovir, there was a potent antiviral effect with a significant reduction in viral load and symptoms compared to placebo. Sisunatovir exhibited a mean IC50 of 1.2 nM against a panel of RSV A and B laboratory strains and clinical isolates with antiviral efficacy in the Balb/C mouse model of RSV infection. Oral bioavailability of sisunatovir in preclinical species ranged from 42 to >100% with evidence of highly efficient penetration into lung tissue. Reference: J Med Chem. 2021 Apr 8;64(7):3658-3676. https://pubmed.ncbi.nlm.nih.gov/33729773/
Solvent mg/mL mM comments
Solubility
DMSO 25.0 56.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 446.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Cockerill GS, Angell RM, Bedernjak A, Chuckowree I, Fraser I, Gascon-Simorte J, Gilman MSA, Good JAD, Harland R, Johnson SM, Ludes-Meyers JH, Littler E, Lumley J, Lunn G, Mathews N, McLellan JS, Paradowski M, Peeples ME, Scott C, Tait D, Taylor G, Thom M, Thomas E, Villalonga Barber C, Ward SE, Watterson D, Williams G, Young P, Powell K. Discovery of Sisunatovir (RV521), an Inhibitor of Respiratory Syncytial Virus Fusion. J Med Chem. 2021 Apr 8;64(7):3658-3676. doi: 10.1021/acs.jmedchem.0c01882. Epub 2021 Mar 17. PMID: 33729773. 2. DeVincenzo J, Tait D, Efthimiou J, Mori J, Kim YI, Thomas E, Wilson L, Harland R, Mathews N, Cockerill S, Powell K, Littler E. A Randomized, Placebo-Controlled, Respiratory Syncytial Virus Human Challenge Study of the Antiviral Efficacy, Safety, and Pharmacokinetics of RV521, an Inhibitor of the RSV-F Protein. Antimicrob Agents Chemother. 2020 Jan 27;64(2):e01884-19. doi: 10.1128/AAC.01884-19. PMID: 31712214; PMCID: PMC6985722.
In vitro protocol:
To be determined
In vivo protocol:
1. Cockerill GS, Angell RM, Bedernjak A, Chuckowree I, Fraser I, Gascon-Simorte J, Gilman MSA, Good JAD, Harland R, Johnson SM, Ludes-Meyers JH, Littler E, Lumley J, Lunn G, Mathews N, McLellan JS, Paradowski M, Peeples ME, Scott C, Tait D, Taylor G, Thom M, Thomas E, Villalonga Barber C, Ward SE, Watterson D, Williams G, Young P, Powell K. Discovery of Sisunatovir (RV521), an Inhibitor of Respiratory Syncytial Virus Fusion. J Med Chem. 2021 Apr 8;64(7):3658-3676. doi: 10.1021/acs.jmedchem.0c01882. Epub 2021 Mar 17. PMID: 33729773. 2. DeVincenzo J, Tait D, Efthimiou J, Mori J, Kim YI, Thomas E, Wilson L, Harland R, Mathews N, Cockerill S, Powell K, Littler E. A Randomized, Placebo-Controlled, Respiratory Syncytial Virus Human Challenge Study of the Antiviral Efficacy, Safety, and Pharmacokinetics of RV521, an Inhibitor of the RSV-F Protein. Antimicrob Agents Chemother. 2020 Jan 27;64(2):e01884-19. doi: 10.1128/AAC.01884-19. PMID: 31712214; PMCID: PMC6985722.
1: Cockerill GS, Angell RM, Bedernjak A, Chuckowree I, Fraser I, Gascon-Simorte J, Gilman MSA, Good JAD, Harland R, Johnson SM, Ludes-Meyers JH, Littler E, Lumley J, Lunn G, Mathews N, McLellan JS, Paradowski M, Peeples ME, Scott C, Tait D, Taylor G, Thom M, Thomas E, Villalonga Barber C, Ward SE, Watterson D, Williams G, Young P, Powell K. Discovery of Sisunatovir (RV521), an Inhibitor of Respiratory Syncytial Virus Fusion. J Med Chem. 2021 Mar 17. doi: 10.1021/acs.jmedchem.0c01882. Epub ahead of print. PMID: 33729773. 2: DeVincenzo J, Tait D, Efthimiou J, Mori J, Kim YI, Thomas E, Wilson L, Harland R, Mathews N, Cockerill S, Powell K, Littler E. A Randomized, Placebo- Controlled, Respiratory Syncytial Virus Human Challenge Study of the Antiviral Efficacy, Safety, and Pharmacokinetics of RV521, an Inhibitor of the RSV-F Protein. Antimicrob Agents Chemother. 2020 Jan 27;64(2):e01884-19. doi: 10.1128/AAC.01884-19. PMID: 31712214; PMCID: PMC6985722. 3: Sevendal ATK, Hurley S, Bartlett AW, Rawlinson W, Walker GJ. Systematic Review of the Efficacy and Safety of RSV-Specific Monoclonal Antibodies and Antivirals in Development. Rev Med Virol. 2024 Sep;34(5):e2576. doi: 10.1002/rmv.2576. PMID: 39209729.