Art. -Nr.: HY-13784

Pirodavir

(Synonyms: R77975)

3 Cited Publications

Kundenbewertung

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).

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Reinheit: 98.41%
CAS. Nr.: 124436-59-5
Formel: C₂₁H₂₇N₃O₃
Molecular Weight:369.46

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Pirodavir Chemical Structure

CAS. Nr.: 124436-59-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Rhinovirus^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	EC₅₀	0.02 μM Compound: Pirodavir	Antiviral activity using H1HeLa cells (ATCC) infected with HRV-14 (range) Antiviral activity using H1HeLa cells (ATCC) infected with HRV-14 (range)	[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	[PMID: 24900468]
HeLa	EC₅₀	0.004 μg/mL Compound: 2	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	[PMID: 24900468]
HeLa	EC₅₀	11.1 ng/mL Compound: 2	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	[PMID: 24900468]
HeLa	EC₅₀	2.3 ng/mL Compound: 2	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	[PMID: 24900468]
HeLa	EC₅₀	2.6 ng/mL Compound: 2	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	[PMID: 24900468]
HeLa	EC₅₀	20.6 ng/mL Compound: 2	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	[PMID: 24900468]
HeLa	EC₅₀	4 ng/mL Compound: 2	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	[PMID: 24900468]
HeLa	EC₅₀	5.6 ng/mL Compound: 2	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	[PMID: 24900468]
KB	CC₅₀	>1 μg/mL Compound: 3	Cellular toxicity against KB cells in HRV-14 strain Cellular toxicity against KB cells in HRV-14 strain	[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	[PMID: 19091578]
KB	CC₅₀	>10 μg/mL Compound: pirodavir	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	[PMID: 19091578]
KB	EC₅₀	<0.0032 μg/mL Compound: pirodavir	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	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]

In Vitro

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

CAS. Nr. 124436-59-5
Appearance Solid
Molecular Weight 369.46
Formel C₂₁H₂₇N₃O₃
Color Light yellow to yellow
SMILES

O=C(OCC)C1=CC=C(OCCC2CCN(C3=NN=C(C)C=C3)CC2)C=C1
Synonyms

R77975
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Nanoscale

Mechanical stiffening of human rhinovirus by cavity-filling antiviral drugs. [Abstract]

2018 Jan 18;10(3):1440-1452. PMID: 29302674
Microorganisms

In Vitro Characterization and Antiviral Susceptibility of Ophidian Serpentoviruses. [Abstract]

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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7067 mL

13.5333 mL

27.0665 mL

5 mM

0.5413 mL

2.7067 mL

5.4133 mL

10 mM

0.2707 mL

1.3533 mL

2.7067 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1 mg/mL (2.71 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Cell Assay^[2]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Pirodavir

3 Cited Publications

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Pirodavir

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Publications Citing Use of MedChemExpress (MCE) Pirodavir

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Pirodavir

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Infection Compound Library

Clinical Compound Library

Antiviral Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Pirodavir

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Pirodavir Related Classifications

HY-13784 Related Classifications