Uprifosbuvir
Based on 1 Customer Validation
Uprifosbuvir (IDX21437; MK-3682) is a nucleotide analog inhibitor that inhibits YFV NS5 RNA-dependent RNA polymerase (RNA polymerase) and HCV NS5b. Uprifosbuvir can be used for research on yellow fever and chronic hepatitis C virus (HCV) 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 : 98.17%
- CAS 番号: 1496551-77-9
- 分子式: C22H29ClN3O9P
- 分子量:545.91
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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
製品説明
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7.5 | EC50 |
1.1 μM
|
Antiviral activity against YFV 17D original in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
Antiviral activity against YFV 17D original in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
|
41765050 |
| Huh-7.5 | EC50 |
9.5 μM
|
Antiviral activity against YFV 17D variant YFV-sof in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
Antiviral activity against YFV 17D variant YFV-sof in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
|
41765050 |
| Huh-7.5 | EC50 |
11.9 μM
|
Antiviral activity against YFV 17D variant YFV-upr in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
Antiviral activity against YFV 17D variant YFV-upr in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
|
41765050 |
| Huh-7.5 | EC50 |
2.1 μM
|
Antiviral activity against YFV 17D reverse-engineered NS5 mutant YFV^M478K in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
Antiviral activity against YFV 17D reverse-engineered NS5 mutant YFV^M478K in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
|
41765050 |
| Huh-7.5 | EC50 |
5.9 μM
|
Antiviral activity against YFV 17D reverse-engineered NS5 mutant YFV^A482G in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
Antiviral activity against YFV 17D reverse-engineered NS5 mutant YFV^A482G in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
|
41765050 |
| Huh-7.5 | EC50 |
12.4 μM
|
Antiviral activity against YFV 17D reverse-engineered NS5 double mutant YFV^M478K+A482G in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
Antiviral activity against YFV 17D reverse-engineered NS5 double mutant YFV^M478K+A482G in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
|
41765050 |
| Huh-7.5 | EC50 |
1.2 μM
|
Antiviral activity against YFV 17D reverse-engineered NS5 mutant YFV^V360L in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
Antiviral activity against YFV 17D reverse-engineered NS5 mutant YFV^V360L in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
|
41765050 |
| Huh-7.5 | EC50 |
2.6 μM
|
Antiviral activity against YFV 17D reverse-engineered NS5 mutant YFV^V607I in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
Antiviral activity against YFV 17D reverse-engineered NS5 mutant YFV^V607I in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
|
41765050 |
| Huh-7.5 | EC50 |
1.4 μM
|
Antiviral activity against YFV 17D reverse-engineered NS5 double mutant YFV^V360L+V607I in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
Antiviral activity against YFV 17D reverse-engineered NS5 double mutant YFV^V360L+V607I in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
|
41765050 |
| Huh-7.5 | EC50 |
1.6 μM
|
Antiviral activity against YFV 17D reverse-engineered NS5 mutant YFV^L720M in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
Antiviral activity against YFV 17D reverse-engineered NS5 mutant YFV^L720M in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
|
41765050 |
| Huh-7.5 | EC50 |
10.8 μM
|
Antiviral activity against YFV 17D reverse-engineered NS5 triple mutant YFV^M478K+A482G+L720M in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
Antiviral activity against YFV 17D reverse-engineered NS5 triple mutant YFV^M478K+A482G+L720M in human hepatoma Huh7.5 cells assessed by virus antigen quantification after 72 hrs incubation.
|
41765050 |
体外実験
Uprifosbuvir (1.5-fold serial dilutions; 72 h) inhibits YFV 17D in Huh7.5 cells with an EC50 of 1.1 μM, and the combined M478K + A482G substitution increases the uprifosbuvir EC50 to 12.4 μM (11.1-fold)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1496551-77-9
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性状 Solid
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分子量 545.91
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分子式 C22H29ClN3O9P
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Color White to off-white
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SMILES
C[C@]([C@@](N(C=CC1=O)C(N1)=O)([H])O[C@@H]2CO[P@@](OC3=CC=CC=C3)(N[C@H](C)C(OC(C)C)=O)=O)([C@@H]2O)Cl
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別名
IDX21437; MK-3682
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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
体外:
DMSO : 250 mg/mL (457.95 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)
プロトコル
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
純度とドキュメンテーション
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データシート (279 KB)
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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)
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取扱説明書 (2659 KB)
参考文献
[1]. Binderup A, et al. Substitutions M478K and A482G in the polymerase of yellow fever virus confer resistance to sofosbuvir and uprifosbuvir in vitro. Antiviral research. 2026 May;249:106381. [Content Brief]
[2]. Klapars A, et al. Efficient synthesis of antiviral agent uprifosbuvir enabled by new synthetic methods. Chemical science. 2021 Jul 07;12(26):9031-9036. [Content Brief]
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 | 1.8318 mL | 9.1590 mL | 18.3180 mL | 45.7951 mL |
| 5 mM | 0.3664 mL | 1.8318 mL | 3.6636 mL | 9.1590 mL | |
| 10 mM | 0.1832 mL | 0.9159 mL | 1.8318 mL | 4.5795 mL | |
| 15 mM | 0.1221 mL | 0.6106 mL | 1.2212 mL | 3.0530 mL | |
| 20 mM | 0.0916 mL | 0.4580 mL | 0.9159 mL | 2.2898 mL | |
| 25 mM | 0.0733 mL | 0.3664 mL | 0.7327 mL | 1.8318 mL | |
| 30 mM | 0.0611 mL | 0.3053 mL | 0.6106 mL | 1.5265 mL | |
| 40 mM | 0.0458 mL | 0.2290 mL | 0.4580 mL | 1.1449 mL | |
| 50 mM | 0.0366 mL | 0.1832 mL | 0.3664 mL | 0.9159 mL | |
| 60 mM | 0.0305 mL | 0.1527 mL | 0.3053 mL | 0.7633 mL | |
| 80 mM | 0.0229 mL | 0.1145 mL | 0.2290 mL | 0.5724 mL | |
| 100 mM | 0.0183 mL | 0.0916 mL | 0.1832 mL | 0.4580 mL |