| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
The primary target of orysastrobin is the mitochondrial cytochrome bc1 complex in fungi. It acts as a QoI fungicide by binding to the Qo site of the cytochrome bc1 complex, inhibiting mitochondrial respiration. This binding blocks electron transfer from cytochrome b to cytochrome c1, disrupting ATP production and cutting off the fungal energy cycle. The compound specifically impairs the oxidation of reduced ubiquinone at the outer side of the cytochrome bc1 site in the electron transfer chains of fungal mitochondria.
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|---|---|
| ln Vitro |
In vitro studies have demonstrated the potent fungicidal activity of orysastrobin against rice pathogens. The compound is a QoI-type fungicide that effectively targets fungal respiration. Orysastrobin has been shown to be highly effective against Magnaporthe oryzae, Pyricularia oryzae, Thanatephorus cucumeris, and Rhizoctonia solani. Its in vitro efficacy makes it a valuable tool for controlling fungal diseases in agricultural settings.
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| ln Vivo |
In vivo studies have confirmed the excellent fungicidal effect of orysastrobin against rice leaf blast, ear blast, and sheath blight. The compound provides protective and curative effects in rice cultivation. Orysastrobin has been developed as a commercial fungicide for agricultural use. Its in vivo efficacy has been demonstrated in field applications, making it an important tool for rice disease management.
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| Enzyme Assay |
For fungicidal activity screening, standard in vitro assays are used to evaluate orysastrobin against fungal pathogens. Fungi are cultured on appropriate media and exposed to serial dilutions of the compound. Mycelial growth inhibition is measured, and EC₅₀ values are calculated. For target identification, biochemical assays using isolated mitochondria or cytochrome bc1 complex are employed to measure respiratory inhibition.
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| Cell Assay |
For in vitro cell-based studies, fungal cells such as Magnaporthe oryzae are cultured in appropriate media. Cells are treated with serial dilutions of orysastrobin, and fungal growth is assessed by measuring colony diameter or optical density. Respiratory activity may be measured using oxygen consumption assays. Standard protocols for fungicidal activity screening are described in the literature.
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| Animal Protocol |
In vivo animal studies for orysastrobin are not applicable as the compound is a fungicide for agricultural use. Efficacy studies are conducted in greenhouse or field settings using rice plants infected with fungal pathogens. Plants are treated with the compound, and disease severity is assessed. Standard protocols for fungicide efficacy testing in plants are followed.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of orysastrobin have not been extensively characterized for mammalian systems as the compound is an agricultural fungicide. Its environmental fate, including persistence and degradation in soil and water, has been studied. The compound's stability and residue levels in crops are important considerations for agricultural use. Specific mammalian PK parameters have not been reported.
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| Toxicity/Toxicokinetics |
Toxicological data for orysastrobin are available from regulatory submissions for agricultural chemicals. As a fungicide, it has been evaluated for environmental and mammalian toxicity. Standard toxicology studies including acute toxicity, repeated-dose toxicity, and ecotoxicity have been conducted. The compound's safety profile supports its use in agriculture with appropriate handling precautions.
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| References | |
| Additional Infomation |
Orysastrobin is a monocarboxylic acid amide formed by the condensation of the carboxyl group of (2E)-(methoxyimino){2-[(3E,5E,6E)-5-(methoxyimino)-4,6-dimethyl-2,8-dioxa-3,7-diazanon-3,6-dien-1-yl]phenyl}acetic acid with the amino group of methylamine. It is a highly effective rice fungicide, effectively controlling Magnaporthe oryzae, Pyricularia oryzae, Thanatephorus cucumeris, and Rhizoctonia solani. It is also a mitochondrial cytochrome bc1 complex inhibitor and antifungal pesticide. It is an oxime ether, monocarboxylic acid amide, amide fungicide, and methoxyiminoacetamide-type methoxyacrylate antifungal agent.
Orysastrobin is a commercial fungicide developed for rice cultivation. It is a QoI-type fungicide that acts as a quinone outside inhibitor, targeting fungal respiration. The compound has been registered for agricultural use in various countries. Orysastrobin provides excellent control of rice blast and sheath blight. No clinical or therapeutic applications have been reported for this compound. |
| Molecular Formula |
C18H25N5O5
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|---|---|
| Molecular Weight |
391.42
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| Exact Mass |
391.186
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| CAS # |
248593-16-0
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| PubChem CID |
11486133
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.16g/cm3
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| Index of Refraction |
1.53
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| LogP |
2.54
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
28
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| Complexity |
630
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CO/N=C(\C(\C)=N\OCC1=C(/C(/C(/O)=N/C)=N\OC)C=CC=C1)/C(/C)=N/OC
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| InChi Key |
JHIPUJPTQJYEQK-ZLHHXESBSA-N
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| InChi Code |
InChI=1S/C18H25N5O5/c1-12(20-25-4)16(22-26-5)13(2)21-28-11-14-9-7-8-10-15(14)17(23-27-6)18(24)19-3/h7-10H,11H2,1-6H3,(H,19,24)/b20-12+,21-13+,22-16+,23-17+
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| Chemical Name |
(2E)-2-[2-[[(E)-[(3E,4E)-3,4-bis(methoxyimino)pentan-2-ylidene]amino]oxymethyl]phenyl]-2-methoxyimino-N-methylacetamide
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5548 mL | 12.7740 mL | 25.5480 mL | |
| 5 mM | 0.5110 mL | 2.5548 mL | 5.1096 mL | |
| 10 mM | 0.2555 mL | 1.2774 mL | 2.5548 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.
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