| CAS NO: | 1191237-69-0 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| 10g | 电议 |
| Name: GS-441524 CAS#: 2378280-82-9 (HCl); 2378280-83-0 (sulfate); 1191237-69-0 Chemical Formula: C12H13N5O4 Exact Mass: 291.0968 Molecular Weight: 291.1 | |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In Vitro) | DMSO: ~120 mg/mL (with ultrasonic) |
| Water: Insoluble | |
| Solubility (In Vivo) | 1. 10 mg/mL (34.3 mM) in 5% ethanol, 30% propylene glycol, 45% PEG 400, 20% water (pH 1.5 with HCI) 2. ≥ 2.7 mg/mL (9.4 mM) in 5% DMSO 40% PEG300 5% Tween-80 50% saline 3. ≥ 2.0 mg/mL (7.1 mM) in 10% DMSO 40% PEG300 5% Tween-80 45% saline or in in 10% DMSO 90% (20% SBE-β-CD in saline) 4. ≥ 2.0 mg/mL (7.1 mM) in 10% DMSO 90% (20% SBE-β-CD in saline) 5. ≥ 2.0 mg/mL (7.1 mM) in 10% DMSO 90% corn oil |
| Technical Information | Synonym: Remdesivir metabolite; GS-441524; GS-5734 metabolite; GS 441524; GS441524; GS5734 metabolite; GS 5734 metabolite; Remdesivir-metabolite; GS-5734-metabolite; GS5734-metabolite; GS 5734-metabolite; 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-carbonitrileSMILES Code: N#C[C@@]1(C2=CC=C3C(N)=NC=NN32)O[C@H](CO)[C@@H](O)[C@H]1O |
| In Vitro | In vitro activity: 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. Cell Assay: To determine the toxicity of GS-441524 to CRFK cells, CRFK cells are treated with 100, 33.3, 11.1, 3.7 or 1.2 μM GS-441524 for 24 h. |
|---|---|
| In Vivo | 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. 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. Remdesivi (IV injection) in NHP results in GS-441524 being present in serum at concentrations 1000-fold higher than Remdesivir throughout a 7-day treatment course. |
| Animal model | Cats |
| Formulation & Dosage | 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). |
| References | [1]. 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. [2]. What Do We Know About Remdesivir Drug Interactions? Clin Transl Sci. 2020 May 13;10.1111/cts.12815. [3]. Advantages of the Parent Nucleoside GS-441524 over Remdesivir for Covid-19 Treatment. ACS Med. Chem. Lett. 2020. |
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