VNT-101
Based on 1 Customer Validation
VNT-101 is an orally active influenza A (IAV) inhibitor. VNT-101 disrupts NP-NP PPI to block NP oligomerization and destabilize the viral ribonucleoprotein (RNP) complex, with potent antiviral activity across multiple influenza A subtypes. VNT-101 exhibits EC50 values of 4-5 nM in cellular cytopathic effect (CPE) assay, 4-8 nM in neuraminidase (NA) assay, and 21-45 nM in RNP assay. VNT-101 demonstrates robust in vivo antiviral efficacy in mice infected with lethal H1N1 virus. VNT-101 can be used for the study of influenza A infection.
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。
- 純度: 99.51%
- CAS 番号: 2894060-67-2
- 分子式: C21H23F3N2O6
- 分子量:456.41
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
VNT-101 exhibits potent anti-influenza A virus activity in RNP assay, with EC50 = 45 nM against H1N1/California subtype and EC50 = 21 nM against H3N2/Alaska subtype[1].
VNT-101 shows strong inhibitory effect on viral neuraminidase in NA assay, with EC50 = 8 nM against H1N1/PR8 subtype and EC50 = 4 nM against H3N2/Alaska subtype[1].
VNT-101 effectively suppresses virus-induced cytopathic effect in CPE assay, with EC50 = 5 nM against H1N1/PR8 subtype and EC50 = 4 nM against H3N2/Alaska subtype[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUCinf | Cmax | CL | Vss | T1/2 | Tmax | F |
|---|---|---|---|---|---|---|---|---|---|
| Dog[1] | 0.5 mg/kg | i.v. | 5.35 μM·h | 8.3 μM | 3.42 mL/min/kg | 3.22 L/kg | 16.7 h | / | / |
| Dog[1] | 2 mg/kg | p.o. | 6.38 μM·h | 1.58 μM | / | / | 15.6 h | 0.83 h | 30 % |
| Mice[1] | 20 mg/kg | p.o. | 52.6 μM·h | 35.1 μM | / | / | 1.87 h | 0.5 h | 28 % |
| Mice[1] | 5 mg/kg | i.v. | 46.7 μM·h | 338 μM | 3.91 mL/min/kg | 0.52 L/kg | 4.03 h | / | / |
| Rat[1] | 10 mg/kg | p.o. | 10.2 μM·h | 1.41 μM | / | / | 5.16 h | 2.13 h | 46 % |
| Rat[1] | 100 mg/kg | p.o. | 122 μM·h | 21.6 μM | / | / | 5.65 h | 1.5 h | 54 % |
| Rat[1] | 30 mg/kg | p.o. | 35.4 μM·h | 7.67 μM | / | / | 5.49 h | 0.42 h | 53 % |
| Rat[1] | 5 mg/kg | i.v. | 11.2 μM·h | 49.8 μM | 17.5 mL/min/kg | 1.68 L/kg | 3.77 h | / | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:H1N1/PR8 influenza A virus (1000 pfu in inoculum, twice the LD100) was intranasally infected into Balb/c mice to establish a lethal influenza infection model[1]
-
Dosage:1, 3, 10, 30 mg/kg
-
Administration:oral administration, twice daily for 5 days
-
Result:Exerted effective anti-influenza activity in Balb/c mice infected with H1N1 virus.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 2894060-67-2
-
性状 Solid
-
分子量 456.41
-
分子式 C21H23F3N2O6
-
Color White to off-white
-
SMILES
COC[C@]1(COC[C@H](O1)COC2=CC=C(C(C=C3C(N)=O)=C(C(F)(F)F)NC3=O)C=C2)C
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (219.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (271 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1910 mL | 10.9551 mL | 21.9101 mL | 54.7753 mL |
| 5 mM | 0.4382 mL | 2.1910 mL | 4.3820 mL | 10.9551 mL | |
| 10 mM | 0.2191 mL | 1.0955 mL | 2.1910 mL | 5.4775 mL | |
| 15 mM | 0.1461 mL | 0.7303 mL | 1.4607 mL | 3.6517 mL | |
| 20 mM | 0.1096 mL | 0.5478 mL | 1.0955 mL | 2.7388 mL | |
| 25 mM | 0.0876 mL | 0.4382 mL | 0.8764 mL | 2.1910 mL | |
| 30 mM | 0.0730 mL | 0.3652 mL | 0.7303 mL | 1.8258 mL | |
| 40 mM | 0.0548 mL | 0.2739 mL | 0.5478 mL | 1.3694 mL | |
| 50 mM | 0.0438 mL | 0.2191 mL | 0.4382 mL | 1.0955 mL | |
| 60 mM | 0.0365 mL | 0.1826 mL | 0.3652 mL | 0.9129 mL | |
| 80 mM | 0.0274 mL | 0.1369 mL | 0.2739 mL | 0.6847 mL | |
| 100 mM | 0.0219 mL | 0.1096 mL | 0.2191 mL | 0.5478 mL |