MedKoo Cat#: 564198 | Name: Sisunatovir HCl
Featured New

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 HCl
CAS#1903763-83-6 (HCl)

Theoretical Analysis

MedKoo Cat#: 564198

Name: Sisunatovir HCl

CAS#: 1903763-83-6 (HCl)

Chemical Formula: C23H23ClF4N4O

Exact Mass: 0.0000

Molecular Weight: 482.91

Elemental Analysis: C, 57.21; H, 4.80; Cl, 7.34; F, 15.74; N, 11.60; O, 3.31

Price and Availability

Size Price Availability Quantity
50mg USD 1,250.00 2 Weeks
100mg USD 1,950.00 2 Weeks
200mg USD 3,650.00 2 Weeks
500mg USD 4,950.00 2 Weeks
1g USD 6,950.00 2 Weeks
2g USD 11,950.00 2 Weeks
Show More
Bulk Inquiry
Buy Now
Add to Cart
Synonym
RV521 hydrochloride; RV-521; RV 521; RV521; Sisunatovir HCl; Sisunatovir hydrochloride;
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 hydrochloride
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
SMILES Code
O=C(C12CC1)N(CC3=NC4=CC(CN)=CC=C4N3CCCC(F)(F)F)C5=C2C=CC(F)=C5.[H]Cl
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
>3 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/

Preparing Stock Solutions

The following data is based on the product molecular weight 482.91 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.