| Size | Price | Stock | Qty |
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| Targets |
Tigolaner acts on the γ-aminobutyric acid (GABA)-gated chloride channels and glutamate-gated chloride channels present in the nervous systems of arthropods. It functions as a negative allosteric modulator of these chloride channels, with a binding site distinct from that of fipronil and other phenylpyrazoles. This selective targeting of invertebrate channels over mammalian counterparts underlies its safety profile in the target animal species.
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| ln Vitro |
In vitro, Tigolaner exhibits potent insecticidal activity by inhibiting GABA-gated chloride channels in parasites, leading to hyperexcitation, paralysis, and death of the target ectoparasites. It is effective against flea and tick populations, including those resistant to older insecticide classes such as phenylpyrazoles. The compound shows superior potency compared to other isoxazolines in certain assays, with a favorable off-target selectivity profile.
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| ln Vivo |
In vivo, Tigolaner demonstrates excellent efficacy as a topical spot-on formulation in cats. A single topical administration provides rapid knockdown and sustained killing of fleas (Ctenocephalides felis) and ticks (Ixodes ricinus, Rhipicephalus sanguineus) for up to 13 weeks. The prolonged duration of action is attributed to its low systemic clearance and slow redistribution from the sebaceous glands and skin layers, ensuring continuous exposure of the parasites to the drug.
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| Enzyme Assay |
Non-cell binding assays for Tigolaner are performed using membrane preparations from insect neuronal tissue or recombinant expression systems expressing parasite GABA-gated chloride channels. Radioligand binding studies using [³H]ethynylbiphenyl or similar tracers are conducted to assess the allosteric modulation of the chloride channel. Membranes are incubated with the radioligand and varying concentrations of Tigolaner (0.001-100 μM). Nonspecific binding is determined with excess unlabeled competitor. After incubation, bound and free ligand are separated by filtration, and radioactivity is counted to calculate IC₅₀ and Ki values.
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| Cell Assay |
Cellular assays are performed using insect cell lines or primary neuronal cultures from target parasites. Cells are treated with Tigolaner at concentrations ranging from 0.001-100 μM. The functional activity is assessed by measuring changes in membrane potential using fluorescent voltage-sensitive dyes or by electrophysiological recording of chloride currents. The inhibitory effect on GABA-evoked currents is quantified, and EC₅₀/IC₅₀ values are determined from dose-response curves. Cytotoxicity is evaluated using mammalian cell lines to confirm selectivity.
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| Animal Protocol |
In vivo efficacy studies are conducted in cats (the target species) according to Good Clinical Practice guidelines. Cats are infested with adult fleas and/or ticks on designated days. Tigolaner is administered as a single topical spot-on dose, typically at the recommended therapeutic volume. Flea and tick counts are performed at various time points post-treatment (e.g., 24 hours, 48 hours, and weekly up to 13 weeks). Efficacy is calculated as the percentage reduction in parasite counts compared to untreated control animals, with duration of protection assessed over the full 13-week period.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies in cats show that Tigolaner is well absorbed through the skin after topical application, with peak plasma concentrations reached within 1-2 days. The compound has a molecular weight of 552.81 g/mol and a molecular formula of C₂₁H₁₃ClF₈N₆O. Its lipophilic nature (XLogP3-AA = 4.7) facilitates accumulation in sebaceous glands and skin, providing sustained release. The terminal elimination half-life in cats is approximately 20-30 days, supporting long-lasting efficacy. It is metabolized by hepatic enzymes and excreted primarily via feces.
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| Toxicity/Toxicokinetics |
Toxicological studies in the target species (cats) indicate that Tigolaner has a wide safety margin at the recommended dose. No clinically significant adverse effects have been observed in healthy cats, kittens, or breeding animals. Compared to older compounds like dieldrin and fipronil, Tigolaner exhibits an improved safety profile due to its selective binding to arthropod channels. However, topical application may cause mild transient reactions at the application site. The compound is contraindicated in animals with known hypersensitivity to isoxazolines.
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| References | |
| Additional Infomation |
Tigolaner belongs to the bispyrazole chemical class and is structurally distinct from other isoxazolines. It was developed by Bayer Animal Health and is the active component of Felpreva®, a combination product that also contains the endoparasiticides emodepside and praziquantel, providing comprehensive external and internal parasite control for cats. The international nonproprietary name (INN) is "tigolaner". It is not approved for use in humans and is intended solely for veterinary applications. Tigolaner represents a significant advance in companion animal parasitology due to its unprecedented duration of action.
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| Molecular Formula |
C21H13CLF8N6O
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|---|---|
| Molecular Weight |
552.807750463486
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| Exact Mass |
552.071
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| CAS # |
1621436-41-6
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| Related CAS # |
Tigolaner-d4
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| PubChem CID |
77847513
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| Appearance |
White to off-white solid powder
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| LogP |
4.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
37
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| Complexity |
934
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=CC=C(C2C=NN(C=2)C2=C(C(F)(F)F)C(C(C(F)(F)F)(F)F)=NN2C)C=C1C(NC1(C#N)CC1)=O
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| InChi Key |
TVAJZOVLQZNNCJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H13ClF8N6O/c1-35-17(14(20(25,26)27)15(34-35)19(23,24)21(28,29)30)36-8-11(7-32-36)10-2-3-13(22)12(6-10)16(37)33-18(9-31)4-5-18/h2-3,6-8H,4-5H2,1H3,(H,33,37)
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| Chemical Name |
2-chloro-N-(1-cyanocyclopropyl)-5-[1-[2-methyl-5-(1,1,2,2,2-pentafluoroethyl)-4-(trifluoromethyl)pyrazol-3-yl]pyrazol-4-yl]benzamide
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 : ~25 mg/mL (~45.22 mM)
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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 | 1.8089 mL | 9.0447 mL | 18.0894 mL | |
| 5 mM | 0.3618 mL | 1.8089 mL | 3.6179 mL | |
| 10 mM | 0.1809 mL | 0.9045 mL | 1.8089 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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