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Modoflaner

Cat No.:V53379 Purity: ≥98%
Modoflaner is an antiparasitic agent.
Modoflaner
Modoflaner Chemical Structure CAS No.: 1331922-53-2
Product category: Parasite
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
Other Sizes
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Product Description
Modoflaner is an antiparasitic agent .
Modoflaner is an innovative isophenylamide antiparasitic compound, also classified as a meta-diamide insecticide/acaricide, developed by Mitsui Chemicals Agro in 2018. It is designed for long-term control of external parasites in animals and as a horticultural or agricultural insecticide. The compound's design incorporates iodine and a fluoropyridine group, contributing to its broad-spectrum activity and systemic properties. Modoflaner is approved by the World Health Organization and has a patent expiry date of September 19, 2038.
Biological Activity I Assay Protocols (From Reference)
Targets
Modoflaner primarily targets gamma-aminobutyric acid (GABA)-gated chloride channels in the nervous system of parasites. It functions as a GABA-gated chloride channel blocker, allosterically modulating these channels and leading to increased neuronal excitability, paralysis, and death of target pests. This mechanism of action is characteristic of the meta-diamide class of insecticides.
ln Vitro
Modoflaner demonstrates significant insecticidal activity in vitro against a range of pests. At concentrations of 0.04, 0.2, and 1 μg/cm², it achieved over 90% mortality against ticks and fleas. In vitro injection tests (0.8, 0.16, and 0.32 μg/individual) showed 100% acaricidal activity. In vitro feeding tests at doses of 4, 0.8, 0.16, 0.032, and 0.064 ppm resulted in over 95% flea mortality. At 100 ppm, it exhibited over 70% mortality against Spodoptera litura, diamondback moth, and small brown planthopper.
ln Vivo
Modoflaner exhibits potent in vivo activity as an antiparasitic agent for controlling external parasites in animals, particularly fleas and ticks. It is effective in veterinary applications for pets (cats, dogs), poultry, and ornamental fish. As an agricultural insecticide, it demonstrates in vivo efficacy against lepidopteran pests (e.g., Helicoverpa armigera, rice stem borer, corn borer) and homopteran pests (e.g., planthoppers, aphids) on various crops including fruits, vegetables, and rice.
Enzyme Assay
In vitro enzyme/receptor binding assays for modoflaner typically involve evaluating its interaction with GABA-gated chloride channels. These assays measure the compound's ability to allosterically modulate and block these channels, often using radioligand binding or electrophysiological techniques on insect neuronal membranes. The compound's binding affinity and inhibitory potency can be determined by assessing its effect on chloride ion flux or by measuring displacement of a known channel blocker.
Cell Assay
In vitro cellular assays for modoflaner involve treating cultured insect cells or parasite tissues with varying concentrations of the compound. Efficacy is assessed by measuring cell viability, paralysis, or mortality. For example, assays may use tick or flea cell lines, or primary cultures of insect neurons. The compound's ability to induce neuronal hyperexcitability and subsequent cell death is quantified, and EC50 or LC50 values are determined from dose-response curves.
Animal Protocol
In vivo animal experiments for modoflaner involve administering the compound to animal models infested with parasites (e.g., fleas, ticks) or to crop plants infected with pests. Efficacy is evaluated by measuring parasite mortality, reduction in infestation levels, or protection of crops from pest damage. Studies may involve topical application, oral administration, or injection, followed by monitoring of clinical signs and parasitological outcomes over a defined period.
ADME/Pharmacokinetics
Pharmacokinetic data for modoflaner are not extensively documented. As a lipophilic compound with a molecular weight of 715.23, it is expected to have good tissue penetration and systemic distribution following administration. The compound's long-lasting efficacy suggests a favorable pharmacokinetic profile with sustained exposure at target sites. Further studies are needed to fully characterize its absorption, distribution, metabolism, and excretion (ADME) properties in target animals.
Toxicity/Toxicokinetics
Toxicological data for modoflaner are limited in the available literature. As a meta-diamide insecticide targeting GABA-gated chloride channels, its selectivity for invertebrate versus vertebrate channels contributes to a favorable safety profile for mammals. The compound is intended for veterinary and agricultural use, with no reported human therapeutic applications. Standard safety precautions should be followed when handling this compound in research settings.
References

[1]. International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information, Vol. 34, No. 2, 2020.

[2]. Modoflaner.

Additional Infomation
Modoflaner (CAS#: 1331922-53-2) has the molecular formula C23H10F12IN3O2 and a molecular weight of 715.23. Its IUPAC name is 6-fluoro-N-[2-fluoro-3-[[4-(1,1,1,2,3,3,3-heptafluoropropan-2-yl)-2-iodo-6-(trifluoromethyl)phenyl]carbamoyl]phenyl]pyridine-3-carboxamide. The compound is not an approved therapeutic drug but is a research tool for studying parasite control and insecticidal mechanisms.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H10F12IN3O2
Molecular Weight
715.229719638824
Exact Mass
714.962
CAS #
1331922-53-2
PubChem CID
138490927
Appearance
Typically exists as solid at room temperature
LogP
6.8
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
15
Rotatable Bond Count
5
Heavy Atom Count
41
Complexity
932
Defined Atom Stereocenter Count
0
InChi Key
IUJSREIEVDNHMT-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H10F12IN3O2/c24-15-5-4-9(8-37-15)18(40)38-14-3-1-2-11(16(14)25)19(41)39-17-12(21(27,28)29)6-10(7-13(17)36)20(26,22(30,31)32)23(33,34)35/h1-8H,(H,38,40)(H,39,41)
Chemical Name
6-fluoro-N-[2-fluoro-3-[[4-(1,1,1,2,3,3,3-heptafluoropropan-2-yl)-2-iodo-6-(trifluoromethyl)phenyl]carbamoyl]phenyl]pyridine-3-carboxamide
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : 100 mg/mL (139.82 mM)
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.3982 mL 6.9908 mL 13.9815 mL
5 mM 0.2796 mL 1.3982 mL 2.7963 mL
10 mM 0.1398 mL 0.6991 mL 1.3982 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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