MDL | - |
---|---|
Molecular Weight | 479.53 |
Molecular Formula | C25H29N5O5 |
SMILES | O[C@H]1[C@@H](O)[C@](C#N)(C2=CC=C3C(N)=NC=NN32)O[C@@H]1COC(C(C)C(C=C4)=CC=C4CC(C)C)=O |
ATV041 is an orally active Ibuprofen (HY-78131) and nucleotide analogue. ATV041 improves oral pharmacokinetic (PK) profile and tissue distribution with anti- mouse hepatitis virus (MHV) activity. ATV041 reduces viral load, tissue damage and virus-induced inflammation in a dose-dependent manner [1] .
Mouse hepatitis virus (MHV) [1]
ATV041 inhibits CCoV, FIPV and TGEV with EC 50 values of 1.406 µM, 7.34 µM and 3.777 µM, respectively [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
ATV041 (200 mg/kg; p.o.; single dose) is widely and rapidly distributes in plasma, liver, lung and kidney tissues
[1]
.
ATV041 (10, 50 and 200 mg/kg; p.o.; single dose) inhibits virus replication in liver and lung in a dose-dependent manner. ATV041 down-regulates the expression of TNF-α、IL-1β、IL-6、IFN-γand CXCL10 inflammatory factors and improves tissue damage
[1]
.
Pharmacokinetic (PK) parameters of GS-441524 and Ibuprofen in SD rats
[1]
(GS-441524 and Ibuprofen are produced by hydrolysis of ATV041)
Analytes | Route | Dose (mg/kg) | T 1/2 (h) | T max (h) | C max (µM/L) | AUC 0-∞ (h•µM/L) | MRT 0-∞ (h) | F (%) |
GS-441524 | p.o. | 25.0 | 4.98±3.57 | 0.67±0.29 | 7.75±1.58 | 22.6±2.34 | 3.16±1.21 | 60.31±0.06 |
GS-441524 | i.v. | 5.0 | 2.81±3.28 | 0.08±0.00 | 5.67±0.57 | 7.51±0.85 | 1.28±0.139 | - |
Ibuprofen | p.o. | 25.0 | 2.63±1.78 | 0.67±0.29 | 80.2±12 | 263±37 | 3.35±0.925 | 78.42±0.11 |
Ibuprofen | i.v. | 5.0 | 1.58±0.82 | 0.03±0.00 | 41.8±3.12 | 67.1±4.39 | 1.57±0.294 | - |
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | SD rats [1] |
Dosage: | 5 or 25 mg/kg |
Administration: | Oral gavage or intravenous injection; single dose |
Result: | Showed an oral activity and efficacy. |
Animal Model: | BALB/c mice [1] |
Dosage: | 10, 50 and 200 mg/kg |
Administration: | Oral gavage; single dose |
Result: | Improved tissue distribution and reduced viral load, tissue damage, virus-induced inflammation. |
Room temperature in continental US; may vary elsewhere.
Please store the product under the recommended conditions in the Certificate of Analysis.