Cyclopropavir
Based on 1 Customer Validation
Cyclopropavir (Filociclovir) is an orally active and broad-spectrum anti-herpesvirus compound. Cyclopropavir inhibits UL97 kinase activity. Cyclopropavir has antiviral activity against HCMV, MCMV, and HAdV6 viruses.
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: 98.0%
- CAS 番号: 632325-71-4
- 分子式: C11H13N5O3
- 分子量:263.26
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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
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BSC-1 | EC50 |
>100 μM
Compound: 2b
|
Antiviral activity against Herpes simplex virus type 1 in african green monkey BSC1 cells by ELISA
Antiviral activity against Herpes simplex virus type 1 in african green monkey BSC1 cells by ELISA
|
[PMID: 19410465] |
| CCRF-HSB-2 | CC50 |
>20 μM
Compound: CPV
|
Cytotoxicity against human HSB2 cells after 7 days by Cell-Titer Glo assay
Cytotoxicity against human HSB2 cells after 7 days by Cell-Titer Glo assay
|
[PMID: 22607883] |
| Daudi | CC50 |
>190 μM
Compound: 6b
|
In vitro cytotoxic concentration required to inhibit Epstein-Barr virus (EBV) replication in Daudi cells
In vitro cytotoxic concentration required to inhibit Epstein-Barr virus (EBV) replication in Daudi cells
|
[PMID: 14736238] |
| Daudi | EC50 |
119 μM
Compound: 6b
|
In vitro effective concentration required to inhibit Epstein-Barr virus (EBV) replication in Daudi cells
In vitro effective concentration required to inhibit Epstein-Barr virus (EBV) replication in Daudi cells
|
[PMID: 14736238] |
| Fibroblast | EC50 |
0.46 μM
Compound: 3b
|
Antiviral activity against Human cytomegalovirus Towne infected in human foreskin fibroblast cells by plaque reduction assay
Antiviral activity against Human cytomegalovirus Towne infected in human foreskin fibroblast cells by plaque reduction assay
|
[PMID: 19397271] |
| HepG2 | CC50 |
>50 μM
Compound: 6b
|
In vitro cytotoxic concentration required to inhibit hepatitisB virus (HBV) replication in 2.2.15 cell line
In vitro cytotoxic concentration required to inhibit hepatitisB virus (HBV) replication in 2.2.15 cell line
|
[PMID: 14736238] |
| HFF | CC50 |
>100 μM
Compound: 2b
|
Cytotoxicity against HFF by visual cytotoxicity assay
Cytotoxicity against HFF by visual cytotoxicity assay
|
[PMID: 19410465] |
| HFF | CC50 |
>100 μM
Compound: 3b
|
Cytotoxicity against HFF cells by neutral red uptake assay
Cytotoxicity against HFF cells by neutral red uptake assay
|
[PMID: 19397271] |
| HFF | CC50 |
>100 μM
Compound: 3b
|
Cytotoxicity against HFF cells by plaque reduction assay
Cytotoxicity against HFF cells by plaque reduction assay
|
[PMID: 19397271] |
| HFF | CC50 |
>100 μM
Compound: 6b
|
In vitro cytotoxic concentration required to inhibit towne strain of human cytomegalovirus (HCMV) replication in HFF cell line
In vitro cytotoxic concentration required to inhibit towne strain of human cytomegalovirus (HCMV) replication in HFF cell line
|
[PMID: 14736238] |
| HFF | CC50 |
>300 μM
Compound: CPV
|
Cytotoxicity against human HFF cells after 3 to 8 days by crystal voilet staining
Cytotoxicity against human HFF cells after 3 to 8 days by crystal voilet staining
|
[PMID: 22607883] |
| HFF | CC50 |
>380 μM
Compound: 1a
|
Cytotoxic concentration against AD169 strain of human cytomegalovirus infected HFF cells of human (by neutral red uptake)
Cytotoxic concentration against AD169 strain of human cytomegalovirus infected HFF cells of human (by neutral red uptake)
|
[PMID: 15634003] |
| HFF | CC50 |
>380 μM
Compound: 2b
|
Cytotoxicity against HFF by neutral red uptake assay
Cytotoxicity against HFF by neutral red uptake assay
|
[PMID: 19410465] |
| HFF | CC50 |
>380 μM
Compound: 6b
|
In vitro cytotoxic concentration required to inhibit AD169 strain of human cytomegalovirus (HCMV) replication in HFF cell line
In vitro cytotoxic concentration required to inhibit AD169 strain of human cytomegalovirus (HCMV) replication in HFF cell line
|
[PMID: 14736238] |
| HFF | EC50 |
>357 μM
Compound: 6b
|
In vitro effective concentration required to inhibit varicella zoster virus (VZV) replication in HFF cell line
In vitro effective concentration required to inhibit varicella zoster virus (VZV) replication in HFF cell line
|
[PMID: 14736238] |
| HFF | EC50 |
120 μM
Compound: 6b
|
In vitro effective concentration required to inhibit AD169 strain of human cytomegalovirus (HCMV) replication in HFF cell line
In vitro effective concentration required to inhibit AD169 strain of human cytomegalovirus (HCMV) replication in HFF cell line
|
[PMID: 14736238] |
| HFF | EC50 |
39 μM
Compound: 6b
|
In vitro effective concentration required to inhibit towne strain of human cytomegalovirus (HCMV) replication in HFF cell line
In vitro effective concentration required to inhibit towne strain of human cytomegalovirus (HCMV) replication in HFF cell line
|
[PMID: 14736238] |
| HFF | IC50 |
>100 μM
Compound: CPV
|
Antiviral activity against HSV-1 infected in human HFF cells assessed as reduction in cytopathic effect after 3 days by crystal violet staining
Antiviral activity against HSV-1 infected in human HFF cells assessed as reduction in cytopathic effect after 3 days by crystal violet staining
|
[PMID: 22607883] |
| HFF | IC50 |
>100 μM
Compound: CPV
|
Antiviral activity against HSV-2 infected in human HFF cells assessed as reduction in cytopathic effect after 3 days by crystal violet staining
Antiviral activity against HSV-2 infected in human HFF cells assessed as reduction in cytopathic effect after 3 days by crystal violet staining
|
[PMID: 22607883] |
| HFF | IC50 |
>100 μM
Compound: CPV
|
Antiviral activity against VZV infected in human HFF cells assessed as reduction in cytopathic effect after 7 days by crystal violet staining
Antiviral activity against VZV infected in human HFF cells assessed as reduction in cytopathic effect after 7 days by crystal violet staining
|
[PMID: 22607883] |
| HFF | IC50 |
1.4 μM
Compound: CPV
|
Antiviral activity against HCMV infected in human HFF cells assessed as reduction in cytopathic effect after 8 days by plaque reduction assay
Antiviral activity against HCMV infected in human HFF cells assessed as reduction in cytopathic effect after 8 days by plaque reduction assay
|
[PMID: 22607883] |
| MEF | CC50 |
>380 μM
Compound: 6b
|
In vitro cytotoxic concentration required to inhibit murine cytomegalovirus (MCMV) replication in MEF cell line
In vitro cytotoxic concentration required to inhibit murine cytomegalovirus (MCMV) replication in MEF cell line
|
[PMID: 14736238] |
| MEF | EC50 |
42 μM
Compound: 6b
|
In vitro effective concentration required to inhibit murine cytomegalovirus (MCMV) replication in MEF cell line
In vitro effective concentration required to inhibit murine cytomegalovirus (MCMV) replication in MEF cell line
|
[PMID: 14736238] |
| MOLT-3 | CC50 |
>20 μM
Compound: CPV
|
Cytotoxicity against human MOLT3 cells after 7 days by Cell-Titer Glo assay
Cytotoxicity against human MOLT3 cells after 7 days by Cell-Titer Glo assay
|
[PMID: 22607883] |
| MOLT-3 | IC50 |
8 μM
Compound: CPV
|
Antiviral activity against HHV-6B infected in human Molt3 cells assessed as reduction in viral DNA after 7 days by hybridization assay
Antiviral activity against HHV-6B infected in human Molt3 cells assessed as reduction in viral DNA after 7 days by hybridization assay
|
[PMID: 22607883] |
| WI-38 | CC50 |
>100 μM
Compound: Cyclopropavir
|
Cytotoxicity against human WI38 cells by neutral red assay
Cytotoxicity against human WI38 cells by neutral red assay
|
[PMID: 18285481] |
| WI-38 | EC50 |
>100 μM
Compound: Cyclopropavir
|
Antimicrobial activity against BK polyomavirus ATCC VR837 infected in human WI38 cells assessed as reduction in viral titer after 7 days by PCR analysis
Antimicrobial activity against BK polyomavirus ATCC VR837 infected in human WI38 cells assessed as reduction in viral titer after 7 days by PCR analysis
|
[PMID: 18285481] |
Cyclopropavir exhibits antiviral activity against HCMV in human foreskin fibroblasts (HFFs) and mouse embryo fibroblasts (MEFs)[1].
Cyclopropavir (15 µM) inhibits UL97 kinase activity in COS7 cells transfected with UL97 and pp65-GFP fusion protein, as shown by increased formation of nuclear aggresomes[2].
Cyclopropavir (2.5 µM; 5 days) achieves a shorter half-life compared to Ganciclovir (HY-13637) in HCMV-infected human foreskin fibroblasts (HFFs)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cyclopropavir (10-30 mg/kg; p.o.) prevents mortality, mitigates liver/lung pathology, and reduces viral replication in immunosuppressed Syrian hamsters infected intravenously or intranasally with HAdV6[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 632325-71-4
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性状 Solid
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分子量 263.26
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分子式 C11H13N5O3
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Color White to off-white
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SMILES
OCC(/C1=C/N2C3=C(C(N=C(N)N3)=O)N=C2)(C1)CO
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別名
Filociclovir; ZSM-I-62; MBX-400
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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
DMSO : 33.33 mg/mL (126.60 mM; ultrasonic and warming and heat to 60°C; 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
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データシート (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
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- 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]. Kern ER, et al. In vitro activity and mechanism of action of methylenecyclopropane analogs of nucleosides against herpesvirus replication. Antimicrob Agents Chemother. 2005 Mar;49(3):1039-45. [Content Brief]
[2]. James SH, et al. Cyclopropavir inhibits the normal function of the human cytomegalovirus UL97 kinase. Antimicrob Agents Chemother. 2011 Oct;55(10):4682-91. [Content Brief]
[3]. Gentry BG, et al. Metabolism of cyclopropavir and ganciclovir in human cytomegalovirus-infected cells. Antimicrob Agents Chemother. 2014;58(4):2329-33. [Content Brief]
[4]. Kern ER, et al. Oral activity of a methylenecyclopropane analog, cyclopropavir, in animal models for cytomegalovirus infections. Antimicrob Agents Chemother. 2004 Dec;48(12):4745-53. [Content Brief]
[5]. Toth K, et al. Filociclovir Is a Potent In Vitro and In Vivo Inhibitor of Human Adenoviruses. Antimicrob Agents Chemother. 2020 Oct 20;64(11):e01299-20. [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 | 3.7985 mL | 18.9926 mL | 37.9853 mL | 94.9632 mL |
| 5 mM | 0.7597 mL | 3.7985 mL | 7.5971 mL | 18.9926 mL | |
| 10 mM | 0.3799 mL | 1.8993 mL | 3.7985 mL | 9.4963 mL | |
| 15 mM | 0.2532 mL | 1.2662 mL | 2.5324 mL | 6.3309 mL | |
| 20 mM | 0.1899 mL | 0.9496 mL | 1.8993 mL | 4.7482 mL | |
| 25 mM | 0.1519 mL | 0.7597 mL | 1.5194 mL | 3.7985 mL | |
| 30 mM | 0.1266 mL | 0.6331 mL | 1.2662 mL | 3.1654 mL | |
| 40 mM | 0.0950 mL | 0.4748 mL | 0.9496 mL | 2.3741 mL | |
| 50 mM | 0.0760 mL | 0.3799 mL | 0.7597 mL | 1.8993 mL | |
| 60 mM | 0.0633 mL | 0.3165 mL | 0.6331 mL | 1.5827 mL | |
| 80 mM | 0.0475 mL | 0.2374 mL | 0.4748 mL | 1.1870 mL | |
| 100 mM | 0.0380 mL | 0.1899 mL | 0.3799 mL | 0.9496 mL |