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MedKoo Cat#: 565272 | Name: Baloxavir
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Description:

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

Baloxavir, also known as S 033188, is a selective inhibitor of influenza cap-dependent endonuclease. It has shown therapeutic activity in preclinical models of influenza A and B virus infections, including strains resistant to current antiviral agents.

Chemical Structure

Baloxavir
Baloxavir
CAS#1985605-59-1 (Baloxavir)

Theoretical Analysis

MedKoo Cat#: 565272

Name: Baloxavir

CAS#: 1985605-59-1 (Baloxavir)

Chemical Formula: C24H19F2N3O4S

Exact Mass: 483.1064

Molecular Weight: 483.49

Elemental Analysis: C, 59.62; H, 3.96; F, 7.86; N, 8.69; O, 13.24; S, 6.63

Price and Availability

Size Price Availability Quantity
50mg USD 250.00 2 weeks
100mg USD 450.00 2 weeks
250mg USD 950.00 2 weeks
500mg USD 1,650.00 2 Weeks
1g USD 2,850.00 2 Weeks
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Related CAS #
1985605-59-1 (Baloxavir) 1985606-14-1 (marboxil)
Synonym
Baloxavir; Baloxavir acid; BXA; S-033447; S033447; S 033447
IUPAC/Chemical Name
(R)-12-((S)-7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl)-7-hydroxy-3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione
InChi Key
FIDLLEYNNRGVFR-CTNGQTDRSA-N
InChi Code
InChI=1S/C24H19F2N3O4S/c25-16-6-5-13-15(20(16)26)12-34-18-4-2-1-3-14(18)21(13)29-19-11-33-10-9-27(19)24(32)22-23(31)17(30)7-8-28(22)29/h1-8,19,21,31H,9-12H2/t19-,21+/m1/s1
SMILES Code
O=C1N2[C@](COCC2)([H])N([C@@H]3C4=CC=CC=C4SCC5=C(F)C(F)=CC=C35)N6C1=C(O)C(C=C6)=O
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
Product Data
Certificate of Analysis
View CoA: current batch, Lot#A20O01B08
Safety Data Sheet (SDS)
View Safety Data Sheet (SDS)
Instruction
View handling instruction
Biological target:
Baloxavir is a cap-dependent endonuclease (CEN) inhibitor.
In vitro activity:
BXA (baloxavir acid) inhibited viral RNA transcription via selective inhibition of CEN activity in enzymatic assays, and inhibited viral replication in infected cells without cytotoxicity in cytopathic effect assays. The antiviral activity of BXA was also confirmed in yield reduction assays with seasonal type A and B viruses, including neuraminidase inhibitor-resistant strains. Furthermore, BXA showed broad potency against various subtypes of influenza A viruses (H1N2, H5N1, H5N2, H5N6, H7N9 and H9N2). Additionally, serial passages of the viruses in the presence of BXA resulted in isolation of PA/I38T variants with reduced BXA susceptibility. Phenotypic and genotypic analyses with reverse genetics demonstratde the mechanism of BXA action via CEN inhibition in infected cells. These results revealed the in vitro characteristics of BXA and support clinical use of BXM to treat influenza. Reference: Antiviral Res. 2018 Dec;160:109-117. https://www.sciencedirect.com/science/article/pii/S0166354218303632?via%3Dihub
In vivo activity:
In order to evaluate the effects of BXM (baloxavir marboxil) against A(H7N9) in a lethal infection model, mice were inoculated with 10.4 times of 50% mouse lethal dose (MLD50) of A/Anhui/1/2013 (H7N9). All vehicle-treated mice died within 7 days post-infection (dpi) and mean day to death was 6 days (Fig. 1a). Survival rates of BXM at 0.5, 5, and 50 mg/kg twice a day for 1 day were 90%, 100% and 100%, respectively. When compared to the survival time at 28 dpi, all groups treated with BXM showed significant prolonged survival times compared with the groups administered with vehicle. Dramatic body weight loss after infection was observed in the vehicle-treated control group and reached a 28% decrease at 5 dpi (Fig. 1b and Supplementary Fig. 2). By contrast, BXM significantly prevented body weight loss from day 2 to 5 in a dose-dependent manner. These results indicate that BXM exerts improvements in survival in mice infected with A/Anhui/1/2013 (H7N9). Reference: Sci Rep. 2019 Mar 5;9(1):3466. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6401108/
Solvent mg/mL mM
Solubility
DMSO 41.7 86.19
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 483.49 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. Noshi T, Kitano M, Taniguchi K, Yamamoto A, Omoto S, Baba K, Hashimoto T, Ishida K, Kushima Y, Hattori K, Kawai M, Yoshida R, Kobayashi M, Yoshinaga T, Sato A, Okamatsu M, Sakoda Y, Kida H, Shishido T, Naito A. In vitro characterization of baloxavir acid, a first-in-class cap-dependent endonuclease inhibitor of the influenza virus polymerase PA subunit. Antiviral Res. 2018 Dec;160:109-117. doi: 10.1016/j.antiviral.2018.10.008. Epub 2018 Oct 11. PMID: 30316915. 2. Taniguchi K, Ando Y, Nobori H, Toba S, Noshi T, Kobayashi M, Kawai M, Yoshida R, Sato A, Shishido T, Naito A, Matsuno K, Okamatsu M, Sakoda Y, Kida H. Inhibition of avian-origin influenza A(H7N9) virus by the novel cap-dependent endonuclease inhibitor baloxavir marboxil. Sci Rep. 2019 Mar 5;9(1):3466. doi: 10.1038/s41598-019-39683-4. PMID: 30837531; PMCID: PMC6401108.
In vitro protocol:
1. Noshi T, Kitano M, Taniguchi K, Yamamoto A, Omoto S, Baba K, Hashimoto T, Ishida K, Kushima Y, Hattori K, Kawai M, Yoshida R, Kobayashi M, Yoshinaga T, Sato A, Okamatsu M, Sakoda Y, Kida H, Shishido T, Naito A. In vitro characterization of baloxavir acid, a first-in-class cap-dependent endonuclease inhibitor of the influenza virus polymerase PA subunit. Antiviral Res. 2018 Dec;160:109-117. doi: 10.1016/j.antiviral.2018.10.008. Epub 2018 Oct 11. PMID: 30316915. 2. Taniguchi K, Ando Y, Nobori H, Toba S, Noshi T, Kobayashi M, Kawai M, Yoshida R, Sato A, Shishido T, Naito A, Matsuno K, Okamatsu M, Sakoda Y, Kida H. Inhibition of avian-origin influenza A(H7N9) virus by the novel cap-dependent endonuclease inhibitor baloxavir marboxil. Sci Rep. 2019 Mar 5;9(1):3466. doi: 10.1038/s41598-019-39683-4. PMID: 30837531; PMCID: PMC6401108.
In vivo protocol:
1. Taniguchi K, Ando Y, Nobori H, Toba S, Noshi T, Kobayashi M, Kawai M, Yoshida R, Sato A, Shishido T, Naito A, Matsuno K, Okamatsu M, Sakoda Y, Kida H. Inhibition of avian-origin influenza A(H7N9) virus by the novel cap-dependent endonuclease inhibitor baloxavir marboxil. Sci Rep. 2019 Mar 5;9(1):3466. doi: 10.1038/s41598-019-39683-4. PMID: 30837531; PMCID: PMC6401108.
1: Hayden FG, Sugaya N, Hirotsu N, Lee N, de Jong MD, Hurt AC, Ishida T, Sekino H, Yamada K, Portsmouth S, Kawaguchi K, Shishido T, Arai M, Tsuchiya K, Uehara T, Watanabe A; Baloxavir Marboxil Investigators Group. Baloxavir Marboxil for Uncomplicated Influenza in Adults and Adolescents. N Engl J Med. 2018 Sep 6;379(10):913-923. doi: 10.1056/NEJMoa1716197. PMID: 30184455. 2: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Baloxavir. 2020 Jun 22. PMID: 31643258. 3: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Baloxavir. 2023 Feb 15. PMID: 30601619. 4: Baker DE. Baloxavir Marboxil. Hosp Pharm. 2019 Jun;54(3):165-169. doi: 10.1177/0018578719841044. Epub 2019 Apr 1. PMID: 31205326; PMCID: PMC6535926. 5: Ison MG, Portsmouth S, Yoshida Y, Shishido T, Mitchener M, Tsuchiya K, Uehara T, Hayden FG. Early treatment with baloxavir marboxil in high-risk adolescent and adult outpatients with uncomplicated influenza (CAPSTONE-2): a randomised, placebo-controlled, phase 3 trial. Lancet Infect Dis. 2020 Oct;20(10):1204-1214. doi: 10.1016/S1473-3099(20)30004-9. Epub 2020 Jun 8. PMID: 32526195. 6: Shirley M. Baloxavir Marboxil: A Review in Acute Uncomplicated Influenza. Drugs. 2020 Jul;80(11):1109-1118. doi: 10.1007/s40265-020-01350-8. PMID: 32601915. 7: Baker J, Block SL, Matharu B, Burleigh Macutkiewicz L, Wildum S, Dimonaco S, Collinson N, Clinch B, Piedra PA. Baloxavir Marboxil Single-dose Treatment in Influenza-infected Children: A Randomized, Double-blind, Active Controlled Phase 3 Safety and Efficacy Trial (miniSTONE-2). Pediatr Infect Dis J. 2020 Aug;39(8):700-705. doi: 10.1097/INF.0000000000002747. PMID: 32516282; PMCID: PMC7360097. 8: Kumar D, Ison MG, Mira JP, Welte T, Hwan Ha J, Hui DS, Zhong N, Saito T, Katugampola L, Collinson N, Williams S, Wildum S, Ackrill A, Clinch B, Lee N. Combining baloxavir marboxil with standard-of-care neuraminidase inhibitor in patients hospitalised with severe influenza (FLAGSTONE): a randomised, parallel- group, double-blind, placebo-controlled, superiority trial. Lancet Infect Dis. 2022 May;22(5):718-730. doi: 10.1016/S1473-3099(21)00469-2. Epub 2022 Jan 24. PMID: 35085510. 9: Baloxavir (Xofluza) for post-exposure prophylaxis of influenza. Med Lett Drugs Ther. 2021 Jan 11;63(1615):2-3. PMID: 33646997. 10: Dufrasne F. Baloxavir Marboxil: An Original New Drug against Influenza. Pharmaceuticals (Basel). 2021 Dec 24;15(1):28. doi: 10.3390/ph15010028. PMID: 35056085; PMCID: PMC8779813. 11: Yang T. Baloxavir Marboxil: The First Cap-Dependent Endonuclease Inhibitor for the Treatment of Influenza. Ann Pharmacother. 2019 Jul;53(7):754-759. doi: 10.1177/1060028019826565. Epub 2019 Jan 23. PMID: 30674196. 12: Heo YA. Baloxavir: First Global Approval. Drugs. 2018 Apr;78(6):693-697. doi: 10.1007/s40265-018-0899-1. PMID: 29623652. 13: Abraham GM, Morton JB, Saravolatz LD. Baloxavir: A Novel Antiviral Agent in the Treatment of Influenza. Clin Infect Dis. 2020 Oct 23;71(7):1790-1794. doi: 10.1093/cid/ciaa107. PMID: 32020174. 14: Uyeki TM, Hui DS, Zambon M, Wentworth DE, Monto AS. Influenza. Lancet. 2022 Aug 27;400(10353):693-706. doi: 10.1016/S0140-6736(22)00982-5. PMID: 36030813; PMCID: PMC9411419. 15: Świerczyńska M, Mirowska-Guzel DM, Pindelska E. Antiviral Drugs in Influenza. Int J Environ Res Public Health. 2022 Mar 4;19(5):3018. doi: 10.3390/ijerph19053018. PMID: 35270708; PMCID: PMC8910682. 16: O'Hanlon R, Shaw ML. Baloxavir marboxil: the new influenza drug on the market. Curr Opin Virol. 2019 Apr;35:14-18. doi: 10.1016/j.coviro.2019.01.006. Epub 2019 Mar 8. PMID: 30852344. 17: Govorkova EA, Takashita E, Daniels RS, Fujisaki S, Presser LD, Patel MC, Huang W, Lackenby A, Nguyen HT, Pereyaslov D, Rattigan A, Brown SK, Samaan M, Subbarao K, Wong S, Wang D, Webby RJ, Yen HL, Zhang W, Meijer A, Gubareva LV. Global update on the susceptibilities of human influenza viruses to neuraminidase inhibitors and the cap-dependent endonuclease inhibitor baloxavir, 2018-2020. Antiviral Res. 2022 Apr;200:105281. doi: 10.1016/j.antiviral.2022.105281. Epub 2022 Mar 12. PMID: 35292289; PMCID: PMC9254721. 18: Neuberger E, Wallick C, Chawla D, Castro RC. Baloxavir vs oseltamivir: reduced utilization and costs in influenza. Am J Manag Care. 2022 Mar 1;28(3):e88-e95. doi: 10.37765/ajmc.2022.88786. PMID: 35404552. 19: Lou Y, Liu L, Yao H, Hu X, Su J, Xu K, Luo R, Yang X, He L, Lu X, Zhao Q, Liang T, Qiu Y. Clinical Outcomes and Plasma Concentrations of Baloxavir Marboxil and Favipiravir in COVID-19 Patients: An Exploratory Randomized, Controlled Trial. Eur J Pharm Sci. 2021 Feb 1;157:105631. doi: 10.1016/j.ejps.2020.105631. Epub 2020 Oct 25. PMID: 33115675; PMCID: PMC7585719. 20: Locke SC, Splawn LM, Cho JC. Baloxavir marboxil: a novel cap-dependent endonuclease (CEN) inhibitor for the treatment of acute uncomplicated influenza. Drugs Today (Barc). 2019 Jun;55(6):359-366. doi: 10.1358/dot.2019.55.6.2999889. PMID: 31250840.