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GC376 sodium

Catalog No. T5188 CAS 1416992-39-6

GC376 is an inhibitor of 3C-like proteases (3CLpro) with IC50 values range from 0.49~4.35 μM.

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GC376 sodium, CAS 1416992-39-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 42.00
5 mg	In stock	$ 92.00
10 mg	In stock	$ 133.00
25 mg	In stock	$ 185.00
50 mg	In stock	$ 288.00
100 mg	In stock	$ 433.00
500 mg	In stock	$ 987.00
1 mL * 10 mM (in DMSO)	In stock	$ 113.00

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Purity: 96.56%

Purity: 95%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GC376 is an inhibitor of 3C-like proteases (3CLpro) with IC50 values range from 0.49~4.35 μM.
Targets&IC50	3CLpro:0.49~4.35 μM.
In vitro	GC376 was significantly effective against caliciviruses (NV and MNV-1), coronaviruses (TGEV, FIPV, MHV, 229E, and BCV), and picornaviruses (HRVs 18, 51, and 68, EV71, and PTV), with nanomolar or low micromolar IC50s, except for FCV and HAV. Interestingly, FCV was less sensitive to GC376, with IC50s of 35 μM, respectively [1].
In vivo	GC376 was administered subcutaneously every 12 h at a dose of 15 mg/kg. Results Nineteen of 20 cats treated with GC376 regained outward health within 2 weeks of initial treatment. However, disease signs recurred 1-7 weeks after primary treatment and relapses and new cases were ultimately treated for a minimum of 12 weeks. Relapses no longer responsive to treatment occurred in 13 of these 19 cats within 1-7 weeks of initial or repeat treatment(s) [2].
Cell Research	The toxic dose for 50% cell death (TD50) for each compound was determined for the various cells used in this study. Confluent cells grown in 96-well plates were treated with various concentrations (1 to 500 μM) of each compound for 72 h. Cell cytotoxicity was measured by a CytoTox 96 nonradioactive cytotoxicity assay kit and crystal violet staining. The in vitro therapeutic index was calculated by dividing the TD50 by the IC50 [1].
Animal Research	GC376 was synthesized in a highly pure form and formulated at a concentration of 53 mg/ml in 10% ethanol and 90% polyethylene glycol 400, as described previously. GC376 was administered subcutaneously (SC) at a dosage of 15 mg/kg q12h SC, unless stated otherwise. The effective dosage for cats with experimentally induced FIP was 10 mg/kg/ q12h SC, but the dosage was raised to 15 mg/kg after the first cat (CT01) failed to respond to a lower dose of 10 mg/kg suggested by earlier pharmacokinetic studies. This was a clinical decision based on this one cat's response to treatment [2].

Molecular Weight	507.53
Formula	C21H30N3NaO8S
CAS No.	1416992-39-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (88.66 mM)

References and Literature

1. Kim Y, et al. Broad-spectrum antivirals against 3C or 3C-like proteases of picornaviruses, noroviruses, and coronaviruses. J Virol. 2012 Nov;86(21):11754-62. 2. Pedersen NC, et al. Efficacy of a 3C-like protease inhibitor in treating various forms of acquired feline infectious peritonitis. J Feline Med Surg. 2018 Apr;20(4):378-392. 3. Theerawatanasirikul S, Kuo C J, Phecharat N, et al. Structural-based virtual screening and in vitro assays for small molecules inhibiting the feline coronavirus 3CL protease as a surrogate platform for coronaviruses[J]. Antiviral research,. 2020, 182: 104927. 4. Wang Y C, Yang W H, Yang C S, et al. Structural basis of SARS-CoV-2 main protease inhibition by a broad-spectrum anti-coronaviral drug[J]. American Journal of Cancer Research. 2020, 10(8): 2535. 5. Fu L, Ye F, Feng Y, et al. Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease. Nature communications. 2020, 11(1): 1-8.

Citations

1. Hahn F, Wangen C, Häge S, et al.The Trimeric Artesunate Analog TF27, a Broadly Acting Anti-Infective Model Drug, Exerts Pronounced Anti-SARS-CoV-2 Activity Spanning Variants and Host Cell Types.Pharmaceutics.2022, 15(1): 115. 2. Mohseni N, Royster A, Ren S, et al.A novel compound targets the feline infectious peritonitis virus nucleocapsid protein and inhibits viral replication in cell culture.Journal of Biological Chemistry.2023: 102976. 3. Ye X, Li Y, Guo L, et al.Synthesis and enzymatic inhibition effects of thiazolidinedione 3C-like protease inhibitors.Journal of Chemical Research.2023, 47(1): 17475198231152556. 4. Bai Y, Ye F, Feng Y, et al. Structural basis for the inhibition of the SARS-CoV-2 main protease by the anti-HCV drug narlaprevir. Signal Transduction and Targeted Therapy. 2021, 6(1): 1-3 5. Theerawatanasirikul S, Kuo C J, Phecharat N, et al. Structural-based virtual screening and in vitro assays for small molecules inhibiting the feline coronavirus 3CL protease as a surrogate platform for coronaviruses. Antiviral research, 2020, 182: 104927. 6. Herrmann A, Jungnickl D, Cordsmeier A, et al. Cloning of a Passage-Free SARS-CoV-2 Genome and Mutagenesis Using Red Recombination. International Journal of Molecular Sciences. 2021, 22(19): 10188. 7. Wang Y C, Yang W H, Yang C S, et al. Structural basis of SARS-CoV-2 main protease inhibition by a broad-spectrum anti-coronaviral drug. American Journal of Cancer Research. 2020, 10(8): 2535 8. Fu L, Ye F, Feng Y, et al Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease. Nature communications. 2020 Sep 4;11(1):4417. doi: 10.1038/s41467-020-18233-x. 9. Chen Y, Li X, Wang M, et al.A cysteine protease inhibitor GC376 displays potent antiviral activity against coxsackievirus infection.Current Research in Microbial Sciences.2023: 100203.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max Anti-Infection Compound Library Bioactive Compound Library Preclinical Compound Library Anti-Viral Compound Library Anti-COVID-19 Compound Library NO PAINS Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid 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 master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Keywords

GC376 sodium 1416992-39-6 Microbiology/Virology SARS-CoV GC-376 sodium inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.