Description | GS-441524 could strongly inhibits feline infectious peritonitis virus (FIPV), with an EC50 of 0.78 μM. |
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Related Catalog | Research Areas >> Infection Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis |
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Target | EC50: 0.78 μM (FIPV)[1]. |
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In Vitro | The cells appear and grow normally at all concentrations of GS-441524 and fail to uptake the fluorescent dye CellTox Green at 24 h. The cytotoxic concentration-50% (CC50) is therefore>100 μM. The effective concentration-50% (EC50) of GS-441524 is calculated to be 0.78 μM[1]. |
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In Vivo | All 10 treated cats have a rapid response to treatment and lymphocyte levels and rectal temperatures return to pre-infection levels and levels of the two asymptomatic cats. Two of the 10 treated cats, 16-116 (Group A) and 16-127 (Group B), have recurrences disease at four and six weeks post treatment. These two cats are treated a second time for two weeks and their response is identical to that of primary treatment. All ten of the once or twice treated cats have remained normal to date (more than eight months post infection). Injections cause a transient "stinging" reaction in some cats within 10 s of compound administration. Localized and transient pain is evidenced by unusual posturing, licking at the injection site and/or vocalizations that last for approximately 30-60 s after injection. Injection reactions are more pronounced in some animals relative to others and reactions are inconsistent from one injection to the next and decreas over time[1]. |
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Solvent | In Vitro: DMSO : 125 mg/mL (429.17 mM; Need ultrasonic) In Vivo: 1. Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (7.14 mM); Clear solution
2. Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in saline) Solubility: ≥ 2.08 mg/mL (7.14 mM); Clear solution
3. Add each solvent one by one: 10% DMSO 90% corn oil Solubility: ≥ 2.08 mg/mL (7.14 mM); Clear solution
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Solubility | 1 mM3.4334 mL17.1668 mL34.3336 mL5 mM0.6867 mL3.4334 mL6.8667 mL10 mM0.3433 mL1.7167 mL3.4334 mL |
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Cell Assay | To determine the toxicity of GS-441524 to CRFK cells n, CRFK cells are treated with 100, 33.3, 11.1, 3.7 or 1.2 μM GS-441524 for 24 h[1]. |
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Animal Admin | Cats[1] The 10 cats that developed disease signs are divided into two groups and treated with either 5 mg/kg (Group A; n=5) or 2 mg/kg (Group B; n=5) GS-441524 SC q24 h starting three days after unequivocal clinical evidence of FIP (days 12-19 post infection). The two cats that do not develop disease signs serve as controls for normal blood lymphocyte counts and rectal temperature[1]. |
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Storage | Powder-20°C3 years 4°C2 yearsIn solvent-80°C6 months -20°C1 month |
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Shipping | Room temperature |
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SMILES | N#C[C@@]1(C2=CC=C3N2N=CN=C3N)O[C@H](CO)[C@@H](O)[C@H]1O |
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References | [1]. Murphy BG, et al. The nucleoside analog GS-441524 strongly inhibits feline infectious peritonitis (FIP) virus in tissue culture and experimental cat infection studies. Vet Microbiol. 2018 Jun;219:226-233. |
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