GC376 sodium
Based on 7 publication(s) in Google Scholar
GC376 sodium is a 3CLpro inhibitor; inhibits the replication of viruses TGEV, FIPV and PTV with IC50 values of 0.15, 0.2 and 0.15 μM, respectively.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.53%
- CAS 番号: 1416992-39-6
- 分子式: C21H30N3NaO8S
- 分子量:507.53
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保管条件:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
MedChemExpress(MCE)の使用を引用している文献 GC376 sodium
More- Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]
- Acta Pharm Sin B. 2024 Sep;14(9):4028-4044. [Abstract]
- Nat Prod Bioprospect. 2025 Jun 13;15(1):39. [Abstract]
- Commun Biol. 2022 Sep 16;5(1):976. [Abstract]
- ACS Pharmacol Transl Sci. 2025 Oct 9;8(11):3944-3952. [Abstract]
- Vet Res. 2024 Sep 27;55(1):124. [Abstract]
- University of California. 2023 Jun.
生物活性
製品説明
IC50 & Target
IC50: 0.15 μM (TGEV), 0.2 μM (FIPV), 0.15 μM (PTV), 0.15 μM (229E), 1.1 μM (MHV), 5.3 μM (MNV-1), 0.6 μM (BCV)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero C1008 | CC50 |
>100 μM
Compound: GC376
|
Cytotoxicity against African green monkey GFP tagged Vero E6 cells assessed as reduction in cell viability by measuring fluoroscence in presence of CP1003 at 2 uM after 72 hrs
Cytotoxicity against African green monkey GFP tagged Vero E6 cells assessed as reduction in cell viability by measuring fluoroscence in presence of CP1003 at 2 uM after 72 hrs
|
[PMID: 36332546] |
体外実験
GC376 sodium covalently binds to Cys 139, Cys 147, and Cys 144 of NV 3CLpro, PV 3Cpro, and TGEV 3CLpro, respectively. GC376 sodium is 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 is less sensitive to GC376, with IC50 of 35 μM. GC376 sodium shows no or weak effectiveness against the replication of HAV in cells[1]. Proteases from NV, MD145 or MNV-1 are inhibited by GC376 sodium with a similar potency. The IC50 values of GC376 sodium against 3CLpro from NV, MD145, and MNV-1 are comparable among tested viruses[2]. GC376 sodium effectively inhibits the replication of NPI52-resistant viruses in cell culture as wild-type viruses, indicating that the mutation does not confer cross-resistance to GC376 sodium[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1416992-39-6
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性状 Solid
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分子量 507.53
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分子式 C21H30N3NaO8S
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Color Off-white to yellow
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SMILES
O=C(N[C@@H](CC(C)C)C(N[C@@](C(S(=O)(O[Na])=O)O)([H])CC1C(NCC1)=O)=O)OCC2=CC=CC=C2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (7)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]2025 Dec 15;10(1):406. PMID: 41392286 -
Acta Pharm Sin B
2024 Sep;14(9):4028-4044. PMID: 39309487 -
Nat Prod Bioprospect
Exploring anti-SARS-CoV-2 natural products: dual-viral target inhibition by delphinidin and the anti-coronaviral efficacy of deapio platycodin D. [Abstract]2025 Jun 13;15(1):39. PMID: 40512442 -
Commun Biol
Autoprocessing and oxyanion loop reorganization upon GC373 and nirmatrelvir binding of monomeric SARS-CoV-2 main protease catalytic domain. [Abstract]2022 Sep 16;5(1):976. PMID: 36114420 -
ACS Pharmacol Transl Sci
Development of a Cell-Based Recombinant Green Fluorescent Protein Assay System for Generalized Discovery of Viral Protease Inhibitors. [Abstract]2025 Oct 9;8(11):3944-3952. PMID: 41262580 -
Vet Res
Development and characterization of reverse genetics systems of feline infectious peritonitis virus for antiviral research. [Abstract]2024 Sep 27;55(1):124. PMID: 39334482 -
溶剤 & 溶解度
体外:
H2O : ≥ 100 mg/mL (197.03 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
Kinase Assay[2]
The stock solution (10 mM) of GC376 is prepared in DMSO and further diluted in assay buffer. The final concentrations of DMSO in the assay did not exceed 1.5% (vol/vol). The 3CLpro from NV, MD145 or MNV-1 are incubated with various concentrations (0.01 to 50 µM) of GC376 in 25 µL of assay buffer for 30 min at 37 °C. Following incubation, 25 µL of assay buffer containing substrate is added, and the mixtures are incubated in a 96-well black plate at 37 °C for 60 min. The fluorescence signals are detected using an excitation and emission wavelength of 490 and 520 nm on a fluorescence microplate reader. The RFU are calculated for each well, and the dose-dependent FRET inhibition curves are fitted with variable slope (four parameters) using GraphPad Prism software in order to determine the IC50 values of GC376[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[4]
Twenty cats from 3.3-82 months of age (mean 10.4 months) with various forms of feline infectious peritonitis are accepted into a field trial. Fourteen cats presented with wet or dry-to-wet FIP and six cats presented with dry feline infectious peritonitis. GC376 is administered subcutaneously every 12 h at a dose of 15 mg/kg. Cats with neurologic signs are excluded from the study. Responses to treatment are monitored[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (282 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[2]. Takahashi D, et al. Structural and inhibitor studies of norovirus 3C-like proteases. Virus Res. 2013 Dec 26;178(2):437-44. [Content Brief]
[3]. Yunjeong Kim, et al. Reversal of the Progression of Fatal Coronavirus Infection in Cats by a Broad-Spectrum Coronavirus Protease Inhibitor. PLoS Pathog. 2016 Mar 30;12(3):e1005531. [Content Brief]
[4]. Pedersen NC, et al. Efficacy of a 3C-like protease inhibitor in treating various forms of acquired feline infectious peritonitis. J Feline Med Surg. 2017 Sep 1:1098612X17729626. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.9703 mL | 9.8516 mL | 19.7033 mL | 49.2582 mL |
| 5 mM | 0.3941 mL | 1.9703 mL | 3.9407 mL | 9.8516 mL | |
| 10 mM | 0.1970 mL | 0.9852 mL | 1.9703 mL | 4.9258 mL | |
| 15 mM | 0.1314 mL | 0.6568 mL | 1.3136 mL | 3.2839 mL | |
| 20 mM | 0.0985 mL | 0.4926 mL | 0.9852 mL | 2.4629 mL | |
| 25 mM | 0.0788 mL | 0.3941 mL | 0.7881 mL | 1.9703 mL | |
| 30 mM | 0.0657 mL | 0.3284 mL | 0.6568 mL | 1.6419 mL | |
| 40 mM | 0.0493 mL | 0.2463 mL | 0.4926 mL | 1.2315 mL | |
| 50 mM | 0.0394 mL | 0.1970 mL | 0.3941 mL | 0.9852 mL | |
| 60 mM | 0.0328 mL | 0.1642 mL | 0.3284 mL | 0.8210 mL | |
| 80 mM | 0.0246 mL | 0.1231 mL | 0.2463 mL | 0.6157 mL | |
| 100 mM | 0.0197 mL | 0.0985 mL | 0.1970 mL | 0.4926 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.