| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
The primary molecular target of oxazosulfyl is the ryanodine receptor (RyR) in insects. It binds to insect ryanodine receptors, causing uncontrolled release of calcium ions from intracellular stores, leading to muscle paralysis, feeding cessation, and ultimately insect death. RyR is a well-validated target for diamide insecticides such as chlorantraniliprole.
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| ln Vitro |
In vitro activity is evaluated using insect cell-based calcium flux assays or electrophysiological recordings. Oxazosulfyl stimulates ryanodine binding to insect RyRs with EC50 values in the sub-micromolar range. It induces calcium release from microsomal preparations of insect muscle cells in a concentration-dependent manner, as measured by fluorescent calcium indicators such as Fluo-4 or Fura-2.
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| ln Vivo |
For RyR binding assays, microsomal membranes from insect muscle (e.g., housefly or lepidopteran larvae) are incubated with [3H]ryanodine (5-20 nM) and oxazosulfyl (0.01-1000 nM) in binding buffer (containing 0.3 M KCl, 10 uM CaCl2) for 2 h at 25degC. Bound and free ligand are separated by filtration over Whatman GF/B filters, and radioactivity is counted by liquid scintillation. Specific binding is defined as total binding minus non-specific binding in the presence of 1000-fold excess unlabeled ryanodine.
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| Enzyme Assay |
For cellular assays, insect Sf9 or S2 cells expressing insect ryanodine receptors are loaded with the calcium-sensitive dye Fluo-4-AM (2-5 uM) for 30 min at 25degC. Oxazosulfyl (0.01-1000 nM) is added, and fluorescence intensity (excitation 488 nm, emission 525 nm) is recorded using a fluorescence plate reader to calculate EC50 values. Alternatively, whole-cell patch clamp electrophysiology can be used to measure RyR-mediated calcium currents.
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| Animal Protocol |
In vivo insecticidal activity is evaluated using standard leaf-dip or soil-drench bioassays against agricultural pests such as diamondback moth (Plutella xylostella), beet armyworm (Spodoptera exigua), or aphids. LC50 values are determined by exposing larvae or adults to serial dilutions of oxazosulfyl (0.01-100 mg/L) on treated leaf discs or plants. Mortality is recorded at 24-72 hours post-treatment. Field trials follow standard agricultural protocols.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of oxazosulfyl in insects and plants include rapid uptake and translaminar movement following foliar application. In mammals, it is expected to have moderate oral absorption, with plasma tmax at 1-4 hours post-dose and terminal half-life (t1/2) of 4-12 hours. Hepatic metabolism via CYP450 enzymes is the primary elimination pathway. Minimal bioaccumulation is predicted based on physicochemical properties.
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| Toxicity/Toxicokinetics |
In regulatory toxicology studies required for pesticide registration, oxazosulfyl exhibits low to moderate acute oral toxicity in rodents (LD50 > 500 mg/kg). No significant genotoxicity or mutagenicity was observed in standard Ames tests. Chronic toxicity studies reveal no major organ-specific effects at doses up to 50 mg/kg/day. However, potential risks to aquatic invertebrates and bees have been noted, requiring appropriate environmental safeguards.
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| Additional Infomation |
Oxazosulfyl has received regulatory approval in Japan as a commercial insecticide for agricultural use. It is marketed under various trade names for control of lepidopteran and hemipteran pests in crops such as rice, vegetables, and fruit trees. Its registration status varies by country, with ongoing development in other Asian markets. The product is not intended for human therapeutic use.
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| Molecular Formula |
C15H11F3N2O5S2
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|---|---|
| Molecular Weight |
420.383451700211
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| Exact Mass |
420.006
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| CAS # |
1616678-32-0
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| PubChem CID |
90258515
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| Appearance |
White to off-white solid powder
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| LogP |
2.4
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
745
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PTQBEFQWTBZMED-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H11F3N2O5S2/c1-2-26(21,22)12-4-3-7-19-13(12)14-20-10-8-9(5-6-11(10)25-14)27(23,24)15(16,17)18/h3-8H,2H2,1H3
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| Chemical Name |
2-(3-ethylsulfonylpyridin-2-yl)-5-(trifluoromethylsulfonyl)-1,3-benzoxazole
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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) |
DMSO : ~100 mg/mL (~237.88 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.95 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.5 mg/mL (5.95 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 25.0 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: ≥ 2.5 mg/mL (5.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3788 mL | 11.8940 mL | 23.7880 mL | |
| 5 mM | 0.4758 mL | 2.3788 mL | 4.7576 mL | |
| 10 mM | 0.2379 mL | 1.1894 mL | 2.3788 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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