Pirodavir
Based on 3 publication(s) in Google Scholar
Pirodavir is a potent, broad-spectrum picornavirus inhibitor, and is highly active against both group A and group B rhinovirus serotypes. Pirodavir is very potent in a virus yield reduction assay (IC90=2.3 nM).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.41%
- CAS No.: 124436-59-5
- 화학식: C21H27N3O3
- 분자량:369.46
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Pirodavir
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Biological Activity
Rhinovirus[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | EC50 |
0.02 μM
Compound: Pirodavir
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Antiviral activity using H1HeLa cells (ATCC) infected with HRV-14 (range)
Antiviral activity using H1HeLa cells (ATCC) infected with HRV-14 (range)
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[PMID: 10794684] |
| HeLa | EC50 |
0.003 μg/mL
Compound: 2
|
Antirhinoviral activity against Human rhinovirus 2 infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
Antirhinoviral activity against Human rhinovirus 2 infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
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[PMID: 24900468] |
| HeLa | EC50 |
0.004 μg/mL
Compound: 2
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Antirhinoviral activity against Human rhinovirus 14 infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
Antirhinoviral activity against Human rhinovirus 14 infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
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[PMID: 24900468] |
| HeLa | EC50 |
11.1 ng/mL
Compound: 2
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Antirhinoviral activity against Human rhinovirus B infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
Antirhinoviral activity against Human rhinovirus B infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
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[PMID: 24900468] |
| HeLa | EC50 |
2.3 ng/mL
Compound: 2
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Antirhinoviral activity against minor receptor-resistant Human rhinovirus infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
Antirhinoviral activity against minor receptor-resistant Human rhinovirus infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
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[PMID: 24900468] |
| HeLa | EC50 |
2.6 ng/mL
Compound: 2
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Antirhinoviral activity against antiviral-resistant Human rhinovirus B infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
Antirhinoviral activity against antiviral-resistant Human rhinovirus B infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
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[PMID: 24900468] |
| HeLa | EC50 |
20.6 ng/mL
Compound: 2
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Antirhinoviral activity against antiviral-resistant Human rhinovirus A infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
Antirhinoviral activity against antiviral-resistant Human rhinovirus A infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
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[PMID: 24900468] |
| HeLa | EC50 |
4 ng/mL
Compound: 2
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Antirhinoviral activity against Human rhinovirus A infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
Antirhinoviral activity against Human rhinovirus A infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
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[PMID: 24900468] |
| HeLa | EC50 |
5.6 ng/mL
Compound: 2
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Antirhinoviral activity against major receptor-resistant Human rhinovirus infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
Antirhinoviral activity against major receptor-resistant Human rhinovirus infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
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[PMID: 24900468] |
| KB | CC50 |
>1 μg/mL
Compound: 3
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Cellular toxicity against KB cells in HRV-14 strain
Cellular toxicity against KB cells in HRV-14 strain
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[PMID: 12852746] |
| KB | CC50 |
>10 μg/mL
Compound: pirodavir
|
Cytotoxicity against human KB cells by neutral red uptake assay
Cytotoxicity against human KB cells by neutral red uptake assay
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[PMID: 19091578] |
| KB | CC50 |
>10 μg/mL
Compound: pirodavir
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Cytotoxicity against human KB cells by visual assay
Cytotoxicity against human KB cells by visual assay
|
[PMID: 19091578] |
| KB | EC50 |
<0.0032 μg/mL
Compound: pirodavir
|
Antiviral activity against HRV2 in human KB cells assessed as cytopathic effect by neutral red uptake assay
Antiviral activity against HRV2 in human KB cells assessed as cytopathic effect by neutral red uptake assay
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[PMID: 19091578] |
| KB | EC50 |
<0.0032 μg/mL
Compound: pirodavir
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Antiviral activity against HRV2 in human KB cells assessed as cytopathic effect by visual assay
Antiviral activity against HRV2 in human KB cells assessed as cytopathic effect by visual assay
|
[PMID: 19091578] |
| KB | EC50 |
0.01 μg/mL
Compound: pirodavir
|
Antiviral activity against HRV14 in human KB cells assessed as cytopathic effect by neutral red uptake assay
Antiviral activity against HRV14 in human KB cells assessed as cytopathic effect by neutral red uptake assay
|
[PMID: 19091578] |
| KB | EC50 |
0.081 μg/mL
Compound: pirodavir
|
Antiviral activity against HRV14 in human KB cells assessed as cytopathic effect by visual assay
Antiviral activity against HRV14 in human KB cells assessed as cytopathic effect by visual assay
|
[PMID: 19091578] |
| MRC5 | CC50 |
>50 μg/mL
Compound: 3
|
Cellular toxicity in MRC-5 cells
Cellular toxicity in MRC-5 cells
|
[PMID: 12852746] |
| RD | CC50 |
>100 μM
Compound: R-77975
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Cytotoxicity against human RD cells assessed as reduction in cell viability measured after 24 hrs by MTS/PMS assay
Cytotoxicity against human RD cells assessed as reduction in cell viability measured after 24 hrs by MTS/PMS assay
|
[PMID: 31809045] |
| RD | CC50 |
>100 μM
Compound: Pirodavir
|
Cytotoxicity against human RD cells assessed as reduction in cell viability measured after 3 days by MTS/PMS assay
Cytotoxicity against human RD cells assessed as reduction in cell viability measured after 3 days by MTS/PMS assay
|
[PMID: 34229438] |
| RD | CC50 |
>100 μM
Compound: Pirodavir
|
Cytotoxicity against human RD cells assessed as cell viability measured after 5 days by MTS assay
Cytotoxicity against human RD cells assessed as cell viability measured after 5 days by MTS assay
|
[PMID: 35512567] |
| Vero 76 | CC50 |
>27 μM
Compound: 8
|
Cytotoxicity against monkey Vero 76 cells by microscopic analysis
Cytotoxicity against monkey Vero 76 cells by microscopic analysis
|
[PMID: 33031923] |
| Vero 76 | CC50 |
17 μM
Compound: 8
|
Cytotoxicity against monkey Vero 76 cells by neutral red uptake assay
Cytotoxicity against monkey Vero 76 cells by neutral red uptake assay
|
[PMID: 33031923] |
Pirodavir is a potent, broad-spectrum picornavirus inhibitor. Pirodavir inhibits 80 of the 100 human rhinovirus (HRV) strains tested at a concentration of 64 ng/mL. In that same study, Pirodavir is also effective in inhibiting 16 enteroviruses, with a mean 80% inhibitory concentration (IC80) of 1,300 ng/mL. Pirodavir inhibits enterovirus 71 replication with an IC50 of 5,420 nM and an IC90 of >13,350 nM. Pirodavir inhibits 56 rhinovirus laboratory strains and three of the clinical isolates tested. Pirodavir inhibits 59% of the serotypes and isolates with IC50s of <100 nM[1]. Pirodavir concentrations of 16 and 4μg/mL reduces cell growth by 66% (s.e.m. 0.75) and 28% (s.e.m. 0.25), respectively. Lower concentrations (1μg/mL) of Pirodavir are not inhibitory for cell growth. The 50% cytotoxic concentration of pirodavir for logarithmic cell growth at 37°C is 7μg/mL. Under the conditions of the antiviral assay (confluent HeLa cells at 33°C), the 50% cytotoxic concentration is >50μg/mL[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 124436-59-5
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Appearance Solid
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분자량 369.46
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화학식 C21H27N3O3
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Color Light yellow to yellow
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SMILES
O=C(OCC)C1=CC=C(OCCC2CCN(C3=NN=C(C)C=C3)CC2)C=C1
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Synonyms
R77975
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Nanoscale
2018 Jan 18;10(3):1440-1452. PMID: 29302674 -
Microorganisms
2023 May 24;11(6):1371. PMID: 37374873 -
J Med Virol
Rock1 is a novel host dependency factor of human enterovirus A71: Implication as a drug target. [Abstract]2022 Nov;94(11):5415-5424. PMID: 35791459
용액&용해도
DMSO : 10 mg/mL (27.07 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.71 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.71 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
HeLa cells are seeded at a concentration of approximately 180,000 cells per dish in six-well plates containing 4 mL of growth medium. Growth medium consist of Eagle's basal medium, supplemented with 5% fetal calf serum, 2% sodium bicarbonate, and 1% glutamine. After 24 h of incubation at 37°C in a humidified CO2 atmosphere, the growth medium is removed and replaced by the test solutions (fresh growth medium with or without various concentrations of the antiviral compounds). To assess the cytotoxicity of the antiviral compounds (e.g., Pirodavir), the number of living cells are determined present in triplicate cultures at the time of Pirodavir addition and every 24 h for 3 days. Following trypsinization, the number of viable cells for each drug concentration is counted in triplicate with a Coulter Counter[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Barnard DL, et al. In vitro activity of expanded-spectrum pyridazinyl oxime ethers related to pirodavir: novel capsid-binding inhibitors with potent antipicornavirus activity. Antimicrob Agents Chemother. 2004 May;48(5):1766-72. [Content Brief]
[2]. Andries K, et al. In vitro activity of pirodavir (R 77975), a substituted phenoxy-pyridazinamine with broad-spectrum antipicornaviralactivity. Antimicrob Agents Chemother. 1992 Jan;36(1):100-7. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7067 mL | 13.5333 mL | 27.0665 mL | 67.6663 mL |
| 5 mM | 0.5413 mL | 2.7067 mL | 5.4133 mL | 13.5333 mL | |
| 10 mM | 0.2707 mL | 1.3533 mL | 2.7067 mL | 6.7666 mL | |
| 15 mM | 0.1804 mL | 0.9022 mL | 1.8044 mL | 4.5111 mL | |
| 20 mM | 0.1353 mL | 0.6767 mL | 1.3533 mL | 3.3833 mL | |
| 25 mM | 0.1083 mL | 0.5413 mL | 1.0827 mL | 2.7067 mL |