JMX0312
JMX0312 is a small-molecule salicylamide derivative with submicromolar anti-human adenovirus activity, with an IC50 of 0.18 μM. JMX0312 reduces viral loads in the liver and blood and decreases mortality in immunosuppressed hamsters infected with human adenovirus, and it can be used for research on human adenovirus infection.
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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。
- CAS 番号: 439144-75-9
- 分子式: C14H8ClF4NO2
- 分子量:333.67
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
HAdV-5 0.18 μM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | CC50 |
120.0 μM
|
Cytotoxicity against A549 cells measured via AlamarBlue assay with 48-hour incubation.
Cytotoxicity against A549 cells measured via AlamarBlue assay with 48-hour incubation.
|
32045239 |
| A549 | IC50 |
2.23 μM
|
Inhibition of HAdV-5 entry in A549 cells assessed via GFP expression quantification with 48-hour incubation.
Inhibition of HAdV-5 entry in A549 cells assessed via GFP expression quantification with 48-hour incubation.
|
32045239 |
| A549 | IC50 |
0.18 μM
|
Inhibition of human adenovirus 5 (HAdV-5) replication in A549 cells measured by plaque reduction assay.
Inhibition of human adenovirus 5 (HAdV-5) replication in A549 cells measured by plaque reduction assay.
|
40185285 |
体外実験
JMX0312 (compound 17) potently inhibits the plaque formation of HAdV-5 in 293β5 cells, with an IC50 of 0.18 μM; meanwhile, this compound exhibits low cytotoxicity in A549 cells, with a CC50 of 120.0 μM, and thus has a selectivity index as high as 666.7[1].
JMX0312 (50 μM; 48 h) completely inhibits the entry of HAdV-5 into A549 cells at a concentration of 50 μM. The entry inhibition IC50 in A549 cells is 2.23 μM, and the CC50 is 120.0 μM[1].
JMX0312 (50 μM) reduces the HAdV-5 viral titer in A549 cells by 989-fold[1].
JMX0312 (50 μM; 45 min) does not inhibit the delivery of the HAdV-5 genome to the nucleus under the treatment condition of administration at a concentration of 50 μM with continuous action for 45 min during A549 cell infection[1].
JMX0312 (50 μM; 24 h) does not significantly inhibit HAdV-5 DNA replication in A549 cells when administered at 25 μM for 24 h post-infection[1].
JMX0312 potently inhibits the replication of HAdV-5 in A549 cells, with an IC50 of 0.18 μM, a CC50 of 120.0 μM, and a selectivity index of 666.7[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:50 μM
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Incubation Time:45 min
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Result:Showed no significant difference in the amount of nuclear-associated HAdV genomes compared to the DMSO control.
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Cell Line:A549 cells
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Concentration:50 μM
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Incubation Time:24 h
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Result:Showed low inhibition of HAdV-5 DNA replication compared to the DMSO control.
Parmacokinetics
| Species | Dose | Route | Cmax | T1/2 | AUC0-24 |
|---|---|---|---|---|---|
| Golden hamster[2] | 6.25 mg/kg | i.p. | 0.09 mg/L | 115.47 min | 919.05 mg/min/L |
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:RjHan/AURA (male, 7 weeks old, ~100 g, immunosuppressed with cyclophosphamide, inoculated with HAdV-C6)[2]
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Dosage:6.25 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Did not affect animal body weight.
Reduced liver viral load by 3.55 log10 PFU/g to a mean of 7.44 log10 PFU/g in infected animals (dead or euthanized over 14 days).
Reduced blood viral load by 7.49 log10 PFU/mL to a mean of 6.56 log10 PFU/mL in infected animals (dead or euthanized over 14 days).
Achieved a 14-day survival rate of 50%.
Reduced liver viral load to the assay detection limit of 3.5 log10 PFU/g in animals that survived 14 days.
Reduced blood viral load by 3.44 log10 PFU/mL to a mean of 2.67 log10 PFU/mL, just above the assay detection limit of 2.5 log10 PFU/mL, in animals that survived 14 days.
化学情報
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CAS 番号 439144-75-9
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分子量 333.67
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分子式 C14H8ClF4NO2
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SMILES
O=C(C1=CC(Cl)=CC=C1O)NC2=CC(F)=CC(C(F)(F)F)=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
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)