Jun6504
Jun6504 is an enterovirus 2C inhibitor. Jun6504 shows potent and broad-spectrum antiviral activity against multiple strains of EV-D68 (EC50 = 250 nM), EV-A71 (EC50 = 502.4 nM), and CVB3 (EC50 = 1049 nM). Jun6504 improves paralysis score and weight gain in a neonatal mouse model of EV-D68 infection. Jun6504 reduces viral titers in the spinal cord and the infected quadriceps muscle. Jun6504 can be used for EV-D68 antiviral research.
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。
- 分子式: C18H25N5O
- 分子量:327.42
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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
Jun6504 (1-10000 nM) shows the antiviral activity EC50 values of 250 nM (EV-D68), 502.4 nM (EV-A71) and 1049 nM (CVB3) in RD cells[1]. Jun6504 (1-10000 nM, 60 h) shows antiviral activity against five strains of EVD68 (US/MO114-18947, USMO114-18949, USIL/14-18952, US/L14-18956, USKY114-18953) with EC50 values ranging from 0.25 to 0.47 µM in RD cells[1]. Jun6504 (0.01-10 μM, 3 days) exhibits dose-dependent inhibition against CVA16, CVA6, poliovirus type 1, and CVB3 in CPE assay with EC50 values from 0.24 to 0.57 µM in CPE assay and inhibits EV-A71 and EV-D68 plaque formation in RD cells with EC50 values of 0.22 and 0.13 µM, respectively[1]. Jun6504 (1-1000 μM) displays dose-dependent increases in melting temperatures of the EV-A71, EV-D68, and CVB3 2C proteins[1]. Jun6504 blocks viral replication at an intermediate stage in the viral life cycle evidenced by inhibiting EV-D68 amplification when adds before or at 3 h post-infection (hpi), an effect that can be inhibited when adds at 5 hpi and 7 hpi[1]. Jun6504 (12.8-100 μM) shows the EC50s against P3, P6, and P9 viruses are determined in RD cells as 0.80, 3.38, and 15.45 μM, respectively and shows complete loss of antiviral activity against P7 and P10 viruses, with EC50 values exceeding 30 µM[1]. Jun6504 (0.001-10 μM) exhibits the weakest activity against r2C-I112V/D183V/D323G, with an EC50 of 3.77 µM and shows complete loss of antiviral activity against the EV-D68 2C mutant proteins (F190L, D183V/F190L, D183V/F190L/D323G)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | Tmax | T1/2 | AUCINF_obs | ClF_obs |
|---|---|---|---|---|---|---|---|
| Mice[1] | 50 mg/kg | i.p. | 2.302 ng/mL | 1.2 h | 3.1 h | 11.124 ng·h/mL | 4.5 L/h/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Neonatal mice were infected with EV-D68 by intramuscular injection into the left quadriceps muscle[1]
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Dosage:50 mg/kg
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Administration:i.p. immediately following intramuscular infection once daily for 14 days or i.p. at 24 h post-infection and continued daily for 13 days
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Result:Showed significantly lower paralysis scores and significantly increased body weight gain.
Showed significantly lower viral titers in the spinal cords.
Showed no EV-D68-infected (NeuN+) neurons.
Showed VP2-positive neurons in the lumbar enlargement.
化学情報
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分子量 327.42
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分子式 C18H25N5O
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SMILES
O=C(NCC1(CNC1)C)C2=C(C=NN3C(C)C)C3=NC(C4CC4)=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)