Picarbutrazox 97% TC

Picarbutrazox 97% TC

Details
Active Ingredients: Picarbutrazox
Technical Grade: 97% TC
CAS: 500207-04-5
Appearance: White to off-white crystalline powder 
Certificates: GLP 5 batches, GLP P&C,GLP 6P
Application: Cucumber, melons, watermelon, tomato, potato, brassicas, lettuce, spinach, onion, rice nursery, turfgrass; seed treatment for corn and soybean
Function: Downy mildew, late blight, white rust, and Pythium damping-off/root rot caused by oomycete (water mold) pathogens.
Category
Technical Concentrate
 
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Description
Technical Parameters

Introduction

 

Picarbutrazox 97% TC is a highly effective, oomycete-specific fungicide belonging to the novel tetrazolyloxime (carbamate) class - it is the only commercial compound in this chemical group. Discovered by Dainippon Ink & Chemicals (development code NF-171) and developed by Nippon Soda, it is specifically designed for controlling downy mildew, late blight, and Pythium diseases in vegetables, field crops, and turfgrass.

 

As a high-purity technical material appearing as a white crystalline powder, Picarbutrazox acts by inhibiting the formation of pathogen cell membranes, suppressing mycelial growth and zoospore release, and reducing sporangia formation and oospore germination. It is classified in FRAC Group U17 (unknown mode of action), shows no cross-resistance with carboxylic acid amides (CAA), phenylamides, or QoI fungicides, and provides both protective and curative activity with good translaminar movement.

 

The 97% TC technical material is intended for industrial formulation into commercial fungicide products such as suspension concentrates (SC), water-dispersible granules (WG/WDG), and flowable seed treatments (FS). First registered in Japan in 2017 (Pythilock®), Picarbutrazox is now registered in Japan, the USA, Canada, and China (10% SC, 碧希洛®), and is globally licensed to Syngenta for seed treatment use (Vayantis®). With the compound patent expired in 2022, it has become an attractive new-mode-of-action building block for generic formulation producers.

 

Products Detail

 

Common Name

Picarbutrazox (ISO)

Technical Grade 97% TC (Technical Concentrate)
CAS Number

500207-04-5

Molecular Formula

C20H23N7O3

Molecular Weight

409.44 g/mol

IUPAC Name

tert-butyl (6-{[(Z)-(1-methyl-1H-tetrazol-5-yl)(phenyl)methylene]aminooxymethyl}-2-pyridyl)carbamate

Appearance

White crystalline powder

Density

approx. 1.3 g/cm³ at 25 °C

Melting Point

136.6–138.7 °C

Boiling Point

Decomposes at approx. 150 °C (boiling point not measurable)

Vapor Pressure

<1.2 × 10⁻⁷ Pa at 50 °C

Water Solubility

0.333 mg/L at 20 °C (0.310 mg/L at 10 °C; 0.461 mg/L at 30 °C); readily soluble in acetone, dichloromethane and ethyl acetate

Stability

Stable under normal storage conditions and suitable for long-term industrial formulation

Acute Oral LD50

>2000 mg/kg for rats (low toxicity classification)

Skin & Eye

Slight eye irritation, reversible within 48 h; no skin irritation; not a skin sensitizer; no neurotoxicity, reproductive toxicity, teratogenicity or genotoxicity

ADI (Acceptable Daily Intake)

0.023 mg/kg bw/day (Japan FSCJ; NOAEL 2.34 mg/kg bw/day; no ARfD required)

Ecotoxicity

Carp LC50 (96 h) >363 μg/L; bluegill sunfish LC50 (96 h) >700 μg/L; Daphnia EC50 (48 h) >342 μg/L; green algae >737 μg/L

Target Diseases

Oomycete diseases - downy mildew (Pseudoperonospora cubensis, Plasmopara viticola, Peronospora spp.), late blight (Phytophthora infestans), white rust (Albugo candida) and Pythium damping-off/root rot; suppresses sporangia formation and zoospore release

 

Product Feature and Application

 

As a 97% technical concentrate, Picarbutrazox provides strong protective activity with additional curative and translaminar action against oomycete pathogens. It inhibits cell membrane formation, mycelial growth, and zoospore release of Pythium, Phytophthora, and downy mildew species - including strains resistant to phenylamides and QoI fungicides.

 

For foliar application, it is used at 50–200 g a.i./ha depending on crop, disease, and application method; in China, the 10% SC is registered for cucumber downy mildew at 600–900 mL/ha. For seed treatment, it protects corn and soybean against Pythium seed rot and damping-off (Vayantis®: 2.5–12.5 mL/100 kg seed for corn; 2.5–6.25 mL/100 kg seed for soybean, equal to 1–2.5 g a.i./100 kg seed).

 

Picarbutrazox can be used alone or in rotation and co-formulation with fungicides of different groups (e.g. metalaxyl-M, fludioxonil, sedaxane, tebuconazole) to broaden the disease control spectrum and support resistance management.

 

This 97% TC technical material is intended for industrial formulation into end-use products including:

SC (Suspension Concentrate) - e.g. 10% SC for foliar use

WG / WDG (Water-Dispersible Granules)

FS (Flowable Concentrate) - seed treatment

 

Its stable physicochemical properties, unique mode of action, and formulation flexibility make it an excellent raw material for modern oomycete fungicide production.

 

Target Crops & Diseases

(1)Cucumber – Downy Mildew (Pseudoperonospora cubensis)

Key benefits in cucumber:

Effective control of downy mildew, including CAA- and QoI-resistant populations

Inhibits sporangia and zoospores, interrupting the disease cycle under humid conditions

Protects leaves and extends the harvest period and fruit quality

Picarbutrazox is registered in China (10% SC) for cucumber downy mildew and is widely used in protected cucumber production systems.

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(2)Tomato – Late Blight (Phytophthora infestans)

Key benefits in tomatoes:

Reliable control of late blight in greenhouse and open-field tomatoes

Prevents fruit rot and stem infection during cool, humid weather

Helps maintain fruit quality and market value

Picarbutrazox is commonly used in protected vegetable production systems in Japan.

(3)Potato – Late Blight (Phytophthora infestans)

Key benefits in potatoes:

Strong protection of foliage against late blight epidemics

Reduces tuber infection by suppressing sporangia and zoospore release in the soil

Suitable for rotation programs with phenylamide and CAA fungicides

Picarbutrazox supports integrated late blight management in potato growing regions worldwide.

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(4)Turfgrass – Pythium Blight and Damping-off (Pythium spp.)

Key benefits in turfgrass:

Effective control of Pythium blight on golf courses and sports turf

Protects seedlings against pre- and post-emergence damping-off

New mode of action (FRAC U17) for resistance management in intensive turf programs

In the USA, a 20% WG was registered in 2021 for professional turf Pythium disease control.

Product Qualification

 

  • Production qualification: The production workshop complies with Good Manufacturing Practice (GMP) standards for pesticides and is equipped with professional raw material testing and finished product inspection equipment. Each batch of products undergoes multiple quality control tests.
  • product inspection equipment. Each batch of products undergoes multiple quality control tests.
  • Relative Documents: Third-party authoritative testing institutions shall issue reports, including five-batch; Physical and Chemical; Toxicology.
  • Production capacity: With standardized production lines and comprehensive process control, we ensure stable batch supply of products.

 

Frequently Asked Questions

 

A. What are your MOQ, packaging, lead time and payment terms?

Standard commercial terms for Picarbutrazox 97% TC:

• MOQ: 25 kg (one drum) for trial evaluation; 500 kg for commercial shipments

• Packaging: 25 kg fibre drum with double polyethylene bag and aluminium-foil liner; 25 kg woven bag or 500 kg jumbo bag available on request

• Lead time: 5–7 working days for stock, 15–20 working days for production orders

• Payment: T/T 30% deposit + 70% against B/L copy or discussion by orders.

A 100 g sample is provided free of charge and is dispatched within 7 working days so that your formulation laboratory can start screening immediately.

B. How do you control quality, and what documents come with each batch?

Each batch is tested against a fixed specification: assay ≥97.0% (HPLC), controlled impurity profile, water ≤0.5%, pH of aqueous dispersion, and appearance (white crystalline powder). In-house QC is verified by an independent third-party laboratory.

Documents (not all) supplied with every shipment:

• Certificate of Analysis (assay, impurities, water, pH, mesh) - batch-specific

• Material Safety Data Sheet (MSDS) in English, GHS format

• Retention samples kept for 24 months for traceability

We recommend a pre-shipment sample from the production batch for your own analysis before the first commercial order - this is standard practice for new technical materials.

C. Is your 97% TC technically equivalent to the originator product?

Our material is the same ISO active ingredient (picarbutrazox, CAS 500207-04-5) at a ≥97% technical specification, produced by a documented synthetic route with a controlled impurity profile.

Technical equivalence for generic registration can be supported by the GLP five-batch data, the physico-chemical report and the impurity profile, which are exactly the documents required for a Tier II equivalence assessment in most regulatory systems. Please tell us the destination market and we will confirm which data package applies.

D. Is the product still under patent? Can it be registered as a generic?

The compound patent (originally Dainippon Ink & Chemicals / Nippon Soda) expired on 15 August 2022, so picarbutrazox is available as a generic active ingredient in most markets.

Process and formulation patents held by third parties may still be in force in individual countries. We supply the technical material only; customers are responsible for a freedom-to-operate check in their own market, and we can share the manufacturing route summary under NDA to support that review.

E. In which countries is picarbutrazox already registered?

Key registrations to date:

• Japan (2017) - Pythilock®, vegetables and rice nursery: downy mildew, late blight, Pythium

• USA (2021) - technical material, 20% WG for professional turf Pythium, and seed-treatment products

• Canada (2021) - technical material and Vayantis® seed treatment for corn and soybean (Pythium)

• China (2021) - 97% TC and 10% SC (碧希洛®) for cucumber downy mildew

Further markets, including the EU and Korea, are in the registration pipeline; Brazil has no registration at present. Registration status strongly affects how quickly you can launch, so please confirm your destination market with us before contracting.

F. What regulatory support do you provide for registration in my market?

We support registration at three levels:

• Data package: five-batch GLP report, physico-chemical properties, toxicology, analytical methods (open part of the dossier)

• Access and ownership: Letter of Access (LoA) and data-compensation arrangements for your dossier

• Application support: label text, use-rate rationale, stability data and technical responses to authority questions

For Tier II technical equivalence and local efficacy trials we can also provide reference standards and method validation support.

G. What are the main formulation challenges, and how should we start?

Picarbutrazox has three properties that shape formulation development:

• Very low water solubility (0.333 mg/L at 20 °C) - suspension concentrates require wet milling to D90 3–5 µm with a high-quality polymeric dispersant system (typically 5–10%)

• High lipophilicity (log Pow 4.16) - excellent leaf penetration, but a real risk of crystal growth in SC on storage; an anti-crystallisation additive and a stability test at 54 °C are recommended

• High melting point (136.6–138.7 °C) - well suited to extrusion granulation, but drying temperature in WG production must stay well below the melting point to avoid caking

Starting-point formulations for 10% SC, 20% WG and 36% FS are available under NDA, together with the dispersant and anti-crystallisation recommendations we use in our own development work.

H. Which formulation types and loadings are commercially proven?

• SC 10% - foliar use; the Chinese commercial benchmark for cucumber downy mildew

• WG / WDG 20% - turf and field crops, good for high-humidity markets and bulk handling

• FS 36% - seed treatment; the commercial Vayantis® 3.3 FC delivers 2.5 g a.i./100 kg soybean seed

• Co-formulation packs - with metalaxyl-M, fludioxonil, sedaxane or tebuconazole

Because of the low water solubility, loadings above 20% in SC are difficult without a solvent or a solid formulation; we recommend evaluating 10% SC or 20% WG first.

I. Which products can be co-formulated or tank-mixed with it?

Registered co-formulations on the market today combine picarbutrazox with metalaxyl-M (mefenoxam), fludioxonil, sedaxane and tebuconazole - all with a different FRAC group, which is the main reason for combining them.

For foliar tank mixes (mancozeb, cymoxanil, copper, chlorothalonil), always run a jar test first and avoid strongly alkaline copper formulations and water above pH 8. If you plan a co-formulation, we can supply compatibility and accelerated-stability guidance for the pair you have in mind.

J. How should it be positioned in a resistance management program?

Picarbutrazox is FRAC Group U17 - a mode of action shared with no other commercial fungicide, and with no known cross-resistance to CAA (dimethomorph, mandipropamid), phenylamides (metalaxyl-M) or QoI fungicides.

• Use it where CAA, phenylamide or QoI performance is already declining

• Rotate or mix with a different FRAC group; do not apply it as a stand-alone block all season

• Typical programs use 2–3 applications per season, respecting the local label

K. Why choose picarbutrazox instead of the established oomycete fungicides?

• vs CAA (dimethomorph, mandipropamid) - different target, retains activity on CAA-resistant strains

• vs phenylamides (metalaxyl-M) - no cross-resistance, useful where metalaxyl has lost efficacy

• vs QoI and cyazofamid - independent of the respiratory chain, so it fits QoI-resistant programs

• vs all of them - one active ingredient covering both foliar disease (downy mildew, late blight) and seed/soil Pythium, at a low use rate of 50–200 g a.i./ha

• Patent expired in 2022, so the cost position is now comparable with established actives while the resistance-management value remains intact

 

 

 

 

 

 

 

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