GS-441524 solution
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 555700

CAS#: 1191237-69-0 (solution)

Description: GS-441524 is a potent inhibitor of feline infectious peritonitis (FIP) virus with an EC50 of 0.78 μM.. GS-441524 strongly inhibits feline infectious peritonitis (FIP) virus in tissue culture and experimental cat infection studies. GS-441524 is a molecular precursor to a pharmacologically active nucleoside triphosphate molecule. These analogs act as an alternative substrate and RNA-chain terminator of viral RNA dependent RNA polymerase. Note: This product is supplied as 10mg /mL solution (see additional information for recipe of the solution). Our product GS-441525 solution is for laboratory research use only. It is NOT a FDA approved medicine, and can NOT be used for any treatment or clinical trials! Your order will NOT be fulfilled unless the order is coming from biotech, pharmaceutical-related business, academic or government institutes!

Chemical Structure

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GS-441524 solution
CAS# 1191237-69-0 (solution)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 555700
Name: GS-441524 solution
CAS#: 1191237-69-0 (solution)
Chemical Formula: C12H13N5O4
Exact Mass: 291.10
Molecular Weight: 291.267
Elemental Analysis: C, 49.48; H, 4.50; N, 24.04; O, 21.97

Price and Availability

Size Price Availability Quantity
10mg USD 90 Ready to ship
25mg USD 150 Ready to ship
50mg USD 250 Ready to ship
100mg USD 450 Ready to ship
200mg USD 750 Ready to ship
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Related CAS #: 1191237-69-0 (free base)   2378280-82-9 (HCl)   2378280-83-0 (sulfate)   1191237-69-0 (solution)    

Synonym: GS-441524; GS 441524; GS441524; Remdesivir-metabolite, GS-5734-metabolite; GS5734-metabolite; GS 5734-metabolite;

IUPAC/Chemical Name: (2R,3R,4S,5R)-2-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile

InChi Key: BRDWIEOJOWJCLU-LTGWCKQJSA-N

InChi Code: InChI=1S/C12H13N5O4/c13-4-12(10(20)9(19)7(3-18)21-12)8-2-1-6-11(14)15-5-16-17(6)8/h1-2,5,7,9-10,18-20H,3H2,(H2,14,15,16)/t7-,9-,10-,12+/m1/s1

SMILES Code: N#C[C@@]1(C2=CC=C3C(N)=NC=NN32)O[C@H](CO)[C@@H](O)[C@H]1O

Appearance: clear solution

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: Note: GS-441524 solution was prepared in 10mg /mL followed procedure described in below paper: Pedersen NC, Perron M, Bannasch M, Montgomery E, Murakami E, Liepnieks M, Liu H. Efficacy and safety of the nucleoside analog GS-441524 for treatment of cats with naturally occurring feline infectious peritonitis. J Feline Med Surg. 2019 Apr;21(4):271-281. This paper is available on line: url: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6435921/ Solution composition (all by volume): 5% ethanol, 30% propylene glycol, 45% PEG 400, 20 % water (pH 1.5 with HCl).

Product Data:
Product Data
Instruction:
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Biological target: GS-441524, predominant metabolite of Remdesivir and superior to Remdesivir against Covid-19 , shows comparable efficacy in cell-based models of primary human lung and cat cells infected with coronavirus. GS-441524 could strongly inhibits feline infectious peritonitis virus (FIPV), with an EC50 of 0.78 μM
In vitro activity: GS-441524 inhibited the CPE of SARS-CoV-2 infection in a concentration-dependent manner in Vero E6 cells. The EC50 was 1.86 μM (95% CI of 1.58–2.15 μM), four-fold more potent than that of remdesivir, with an EC50 of 7.43 μM (95% CI of 6.99–7.90 μM). Reference: Front Pharmacol. 2022 Aug 16;13:918083. https://pubmed.ncbi.nlm.nih.gov/36052127/
In vivo activity: Oral treatment with GS-441524 effectively decreased viral RNA loads in feces, blood, and effusion in cats with FIP. Reference: Viruses. 2022 May 17;14(5):1069. https://pubmed.ncbi.nlm.nih.gov/35632813/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 10.0 34.33
DMSO 45.1 154.89
DMF:PBS (pH 7.2) (1:5) 0.2 0.55

Preparing Stock Solutions

The following data is based on the product molecular weight 291.27 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. Wang AQ, Hagen NR, Padilha EC, Yang M, Shah P, Chen CZ, Huang W, Terse P, Sanderson P, Zheng W, Xu X. Preclinical Pharmacokinetics and In Vitro Properties of GS-441524, a Potential Oral Drug Candidate for COVID-19 Treatment. Front Pharmacol. 2022 Aug 16;13:918083. doi: 10.3389/fphar.2022.918083. PMID: 36052127; PMCID: PMC9424906. 2. Doki T, Takahashi K, Hasegawa N, Takano T. In vitro antiviral effects of GS-441524 and itraconazole combination against feline infectious peritonitis virus. Res Vet Sci. 2022 May;144:27-33. doi: 10.1016/j.rvsc.2022.01.005. Epub 2022 Jan 7. PMID: 35033848; PMCID: PMC8739810. 3. Meli ML, Spiri AM, Zwicklbauer K, Krentz D, Felten S, Bergmann M, Dorsch R, Matiasek K, Alberer M, Kolberg L, von Both U, Hartmann K, Hofmann-Lehmann R. Fecal Feline Coronavirus RNA Shedding and Spike Gene Mutations in Cats with Feline Infectious Peritonitis Treated with GS-441524. Viruses. 2022 May 17;14(5):1069. doi: 10.3390/v14051069. PMID: 35632813; PMCID: PMC9147249. 4. Yan VC, Muller FL. Advantages of the Parent Nucleoside GS-441524 over Remdesivir for Covid-19 Treatment. ACS Med Chem Lett. 2020 Jun 23;11(7):1361-1366. doi: 10.1021/acsmedchemlett.0c00316. PMID: 32665809; PMCID: PMC7315846.
In vitro protocol: 1. Wang AQ, Hagen NR, Padilha EC, Yang M, Shah P, Chen CZ, Huang W, Terse P, Sanderson P, Zheng W, Xu X. Preclinical Pharmacokinetics and In Vitro Properties of GS-441524, a Potential Oral Drug Candidate for COVID-19 Treatment. Front Pharmacol. 2022 Aug 16;13:918083. doi: 10.3389/fphar.2022.918083. PMID: 36052127; PMCID: PMC9424906. 2. Doki T, Takahashi K, Hasegawa N, Takano T. In vitro antiviral effects of GS-441524 and itraconazole combination against feline infectious peritonitis virus. Res Vet Sci. 2022 May;144:27-33. doi: 10.1016/j.rvsc.2022.01.005. Epub 2022 Jan 7. PMID: 35033848; PMCID: PMC8739810.
In vivo protocol: 1. Meli ML, Spiri AM, Zwicklbauer K, Krentz D, Felten S, Bergmann M, Dorsch R, Matiasek K, Alberer M, Kolberg L, von Both U, Hartmann K, Hofmann-Lehmann R. Fecal Feline Coronavirus RNA Shedding and Spike Gene Mutations in Cats with Feline Infectious Peritonitis Treated with GS-441524. Viruses. 2022 May 17;14(5):1069. doi: 10.3390/v14051069. PMID: 35632813; PMCID: PMC9147249. 2. Yan VC, Muller FL. Advantages of the Parent Nucleoside GS-441524 over Remdesivir for Covid-19 Treatment. ACS Med Chem Lett. 2020 Jun 23;11(7):1361-1366. doi: 10.1021/acsmedchemlett.0c00316. PMID: 32665809; PMCID: PMC7315846.

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1: Shafer RW. A SARS-CoV-2 antiviral therapy score card. Glob Health Med. 2020 Dec 31;2(6):346-349. doi: 10.35772/ghm.2020.01082. PMID: 33409413; PMCID: PMC7780285.


2: Hanafin PO, Jermain B, Hickey AJ, Kabanov AV, Kashuba AD, Sheahan TP, Rao GG. A Mechanism-based Pharmacokinetic Model of Remdesivir Leveraging Interspecies Scaling to Simulate COVID-19 Treatment in Humans. CPT Pharmacometrics Syst Pharmacol. 2020 Dec 9. doi: 10.1002/psp4.12584. Epub ahead of print. PMID: 33296558.


3: Nili A, Farbod A, Neishabouri A, Mozafarihashjin M, Tavakolpour S, Mahmoudi H. Remdesivir: A beacon of hope from Ebola virus disease to COVID-19. Rev Med Virol. 2020 Nov;30(6):1-13. doi: 10.1002/rmv.2133. Epub 2020 Jul 30. PMID: 33210457.


4: Dickinson PJ. Coronavirus Infection of the Central Nervous System: Animal Models in the Time of COVID-19. Front Vet Sci. 2020 Oct 23;7:584673. doi: 10.3389/fvets.2020.584673. PMID: 33195610; PMCID: PMC7644464.


5: Jung LS, Gund TM, Narayan M. Comparison of Binding Site of Remdesivir and Its Metabolites with NSP12-NSP7-NSP8, and NSP3 of SARS CoV-2 Virus and Alternative Potential Drugs for COVID-19 Treatment. Protein J. 2020 Dec;39(6):619-630. doi: 10.1007/s10930-020-09942-9. Epub 2020 Nov 13. PMID: 33185784; PMCID: PMC7662030.


6: Davis MR, Pham CU, Cies JJ. Remdesivir and GS-441524 plasma concentrations in patients with end-stage renal disease on haemodialysis. J Antimicrob Chemother. 2020 Nov 5:dkaa472. doi: 10.1093/jac/dkaa472. Epub ahead of print. PMID: 33152758.


7: Izes AM, Yu J, Norris JM, Govendir M. Current status on treatment options for feline infectious peritonitis and SARS-CoV-2 positive cats. Vet Q. 2020 Dec;40(1):322-330. doi: 10.1080/01652176.2020.1845917. PMID: 33138721; PMCID: PMC7671703.


8: Sahakijpijarn S, Moon C, Koleng JJ, Christensen DJ, Williams Iii RO. Development of Remdesivir as a Dry Powder for Inhalation by Thin Film Freezing. Pharmaceutics. 2020 Oct 22;12(11):1002. doi: 10.3390/pharmaceutics12111002. PMID: 33105618; PMCID: PMC7690377.


9: Yan VC, Muller FL. Captisol and GS-704277, but Not GS-441524, Are Credible Mediators of Remdesivir's Nephrotoxicity. Antimicrob Agents Chemother. 2020 Nov 17;64(12):e01920-20. doi: 10.1128/AAC.01920-20. PMID: 32988821; PMCID: PMC7674034.


10: Lê MP, Le Beller C, Le Hingrat Q, Jaquet P, Wicky PH, Bunel V, Massias L, Visseaux B, Messika J, Descamps D, Mal H, Timsit JF, Peytavin G. Reply to Yan and Muller, "Captisol and GS-704277, but Not GS-441524, Are Credible Mediators of Remdesivir's Nephrotoxicity". Antimicrob Agents Chemother. 2020 Nov 17;64(12):e01937-20. doi: 10.1128/AAC.01937-20. PMID: 32988815; PMCID: PMC7674048.


11: Paltrinieri S, Giordano A, Stranieri A, Lauzi S. Feline infectious peritonitis (FIP) and coronavirus disease 19 (COVID-19): Are they similar? Transbound Emerg Dis. 2020 Sep 28:10.1111/tbed.13856. doi: 10.1111/tbed.13856. Epub ahead of print. PMID: 32985113; PMCID: PMC7537058.


12: Schooley RT, Carlin AF, Beadle JR, Valiaeva N, Zhang XQ, Garretson AF, Smith VI, Murphy J, Hostetler KY. Rethinking Remdesivir: Synthesis of Lipid Prodrugs that Substantially Enhance Anti-Coronavirus Activity. bioRxiv [Preprint]. 2020 Aug 27:2020.08.26.269159. doi: 10.1101/2020.08.26.269159. PMID: 32869033; PMCID: PMC7457622.


13: Lê MP, Le Hingrat Q, Jaquet P, Wicky PH, Bunel V, Massias L, Visseaux B, Messika J, Descamps D, Mal H, Timsit JF, Peytavin G. Removal of Remdesivir's Metabolite GS-441524 by Hemodialysis in a Double Lung Transplant Recipient with COVID-19. Antimicrob Agents Chemother. 2020 Oct 20;64(11):e01521-20. doi: 10.1128/AAC.01521-20. PMID: 32868327; PMCID: PMC7577145.


14: Pruijssers AJ, George AS, Schäfer A, Leist SR, Gralinksi LE, Dinnon KH 3rd, Yount BL, Agostini ML, Stevens LJ, Chappell JD, Lu X, Hughes TM, Gully K, Martinez DR, Brown AJ, Graham RL, Perry JK, Du Pont V, Pitts J, Ma B, Babusis D, Murakami E, Feng JY, Bilello JP, Porter DP, Cihlar T, Baric RS, Denison MR, Sheahan TP. Remdesivir Inhibits SARS-CoV-2 in Human Lung Cells and Chimeric SARS-CoV Expressing the SARS-CoV-2 RNA Polymerase in Mice. Cell Rep. 2020 Jul 21;32(3):107940. doi: 10.1016/j.celrep.2020.107940. Epub 2020 Jul 7. PMID: 32668216; PMCID: PMC7340027.


15: Yan VC, Muller FL. Advantages of the Parent Nucleoside GS-441524 over Remdesivir for Covid-19 Treatment. ACS Med Chem Lett. 2020 Jun 23;11(7):1361-1366. doi: 10.1021/acsmedchemlett.0c00316. PMID: 32665809; PMCID: PMC7315846.


16: Tempestilli M, Caputi P, Avataneo V, Notari S, Forini O, Scorzolini L, Marchioni L, Ascoli Bartoli T, Castilletti C, Lalle E, Capobianchi MR, Nicastri E, D'Avolio A, Ippolito G, Agrati C; COVID 19 INMI Study Group. Pharmacokinetics of remdesivir and GS-441524 in two critically ill patients who recovered from COVID-19. J Antimicrob Chemother. 2020 Oct 1;75(10):2977-2980. doi: 10.1093/jac/dkaa239. PMID: 32607555; PMCID: PMC7337789.


17: Humeniuk R, Mathias A, Cao H, Osinusi A, Shen G, Chng E, Ling J, Vu A, German P. Safety, Tolerability, and Pharmacokinetics of Remdesivir, An Antiviral for Treatment of COVID-19, in Healthy Subjects. Clin Transl Sci. 2020 Sep;13(5):896-906. doi: 10.1111/cts.12840. Epub 2020 Aug 5. PMID: 32589775; PMCID: PMC7361781.


18: Alvarez JC, Moine P, Etting I, Annane D, Larabi IA. Quantification of plasma remdesivir and its metabolite GS-441524 using liquid chromatography coupled to tandem mass spectrometry. Application to a Covid-19 treated patient. Clin Chem Lab Med. 2020 Jun 22;58(9):1461-1468. doi: 10.1515/cclm-2020-0612. PMID: 32573468.


19: Dickinson PJ, Bannasch M, Thomasy SM, Murthy VD, Vernau KM, Liepnieks M, Montgomery E, Knickelbein KE, Murphy B, Pedersen NC. Antiviral treatment using the adenosine nucleoside analogue GS-441524 in cats with clinically diagnosed neurological feline infectious peritonitis. J Vet Intern Med. 2020 Jul;34(4):1587-1593. doi: 10.1111/jvim.15780. Epub 2020 May 22. PMID: 32441826; PMCID: PMC7379040.


20: Avataneo V, de Nicolò A, Cusato J, Antonucci M, Manca A, Palermiti A, Waitt C, Walimbwa S, Lamorde M, di Perri G, D'Avolio A. Development and validation of a UHPLC-MS/MS method for quantification of the prodrug remdesivir and its metabolite GS-441524: a tool for clinical pharmacokinetics of SARS- CoV-2/COVID-19 and Ebola virus disease. J Antimicrob Chemother. 2020 Jul 1;75(7):1772-1777. doi: 10.1093/jac/dkaa152. PMID: 32361744; PMCID: PMC7197584.