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Purity: ≥98%
Pirodavir (formerly known as R 77975) is the prototype of a novel class of broad-spectrum antipicornavirus compounds. It is a capsid-binding antipicornavirus agent with potent in vitro activity against both group A and group B rhinovirus serotypes. Although its predecessor, R 61837, a substituted phenyl-pyridazinamine, was effective in inhibiting 80% of 100 serotypes tested (EC80) at concentrations above 32 micrograms/ml, pirodavir inhibits the same percentage of viruses at 0.064 micrograms/ml. Pirodavir was one of the most promising capsid-binding compounds to show efficacy in human clinical trials for chemoprophylaxis of the common cold.
| Targets |
Rhinovirus
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| ln Vitro |
Broadly acting picornavirus inhibitor pirodavir is a powerful drug. At a dose of 64 ng/mL, pirodavir inhibits 80 out of the 100 human rhinovirus (HRV) strains that were tested. Pirodavir also demonstrated efficacy against 16 enteroviruses in that study, with a mean 80% inhibitory concentration (IC80) of 1,300 ng/mL. Pirodavir has an IC50 of 5,420 nM and an IC90 of >13,350 nM, which inhibits the replication of enterovirus 71. Three of the tested clinical isolates and 56 rhinovirus laboratory strains are inhibited by pirodavir. 59% of the serotypes and isolates with IC50s of less than 100 nM are inhibited by pirodavir[1].Cell growth is reduced by 66% (s.e.m. 0.75) and 28% (s.e.m. 0.25) at 16 and 4μg/mL, respectively, when pirodavir concentrations are used. Pirodavir does not inhibit cell growth at lower concentrations (1μg/mL). For logarithmic cell growth at 37°C, 7μg/mL is the 50% cytotoxic concentration of pirodavir. 50% cytotoxic concentration is greater than 50μg/mL in the antiviral assay with confluent HeLa cells at 33°C[2].
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| ln Vivo |
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| Cell Assay |
HeLa cells are seeded in six-well plates with 4 mL of growth medium at a density of roughly 180,000 cells per dish. Eagle's basal medium is the growth medium, to which 5% fetal calf serum, 2% sodium bicarbonate, and 1% glutamine are added. The growth medium is removed and replaced with the test solutions (fresh growth medium with or without different concentrations of the antiviral compounds) after a 24-hour incubation period at 37°C in a humidified CO2 atmosphere. The amount of living cells present in triplicate cultures at the time of Pirodavir addition and every 24 hours for three days is counted in order to evaluate the cytotoxicity of the antiviral compounds (e.g., Pirodavir). A Coulter Counter is used to count the number of viable cells in triplicate for each drug concentration after trypsinization[2].
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| Animal Protocol |
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| References |
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| Additional Infomation |
Pirodavir is an antipicornavirus agent.
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| Molecular Formula |
C21H27N3O3
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| Molecular Weight |
369.46
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| Exact Mass |
369.205
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| Elemental Analysis |
C, 68.27; H, 7.37; N, 11.37; O, 12.99
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| CAS # |
124436-59-5
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| Related CAS # |
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| PubChem CID |
71345
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
572.0±40.0 °C at 760 mmHg
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| Melting Point |
124-125℃
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| Flash Point |
299.8±27.3 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.554
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| LogP |
3.94
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
27
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| Complexity |
446
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| Defined Atom Stereocenter Count |
0
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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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| InChi Key |
KCHIOGFOPPOUJC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H27N3O3/c1-3-26-21(25)18-5-7-19(8-6-18)27-15-12-17-10-13-24(14-11-17)20-9-4-16(2)22-23-20/h4-9,17H,3,10-15H2,1-2H3
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| Chemical Name |
Ethyl p-(2-(1-(6-methyl-3-pyridazinyl)-4-piperidyl)ethoxy)benzoate
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| Synonyms |
R 77975; R-77975; R77975; R77,975; R 77,975; R-77,975;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~10 mg/mL (~27.07 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (2.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (2.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 1 mg/mL (2.71 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Chemical structures of capsid-binding picornavirus inhibitors, including the ether oxime derivatives of pirodavir, BTA39 and BTA188.Antimicrob Agents Chemother.2004 May;48(5):1766-72. |
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 Effects of varying the time of addition of compound on the inhibition of HRV-2 (strain HGP) replication in KB cells by pyridazinyl oxime capsid-binding agents. ▪, BTA39; ▴, BTA188; •, pirodavir. Virus was added to the cells at an MOI of 2.Antimicrob Agents Chemother.2004 May;48(5):1766-72. |
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