Sarolaner (Synonyms: PF-6450567) |
Catalog No.GC34774
One-Click Copy Product Info
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Sarolaner is an orally administered, broad-spectrum, isoxazoline ectoparasiticide for dogs.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1398609-39-6
Sample solution is provided at 25 µL, 10mM.
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Sarolaner is an orally administered, broad-spectrum, isoxazoline ectoparasiticide for dogs [1].
In vitro sarolaner demonstrated an LC80 of 0.3μg/mL against C. felis and an LC100 of 0.003μg/mL against O. turicata [1].
In vivo efficacy (> 99%) of sarolaner was demonstrated against fleas and ticks for at least one month from a single oral dose of between 1.25 and 5mg/kg in dogs [1]. Sarolaner at an oral dose of 2mg/kg was highly effective in reducing the live mite counts in dogs with a natural infestation of Demodex spp. and an induced infestation of O. cynotis [2]. Oral administration of sarolaner at 2–4mg/kg achieved >95% efficacy against the feline fur mite Lynxacarus radovskyi at Day 30 post-treatment [3].
References:
[1] McTier, Tom L., et al. "Discovery of sarolaner: A novel, orally administered, broad-spectrum, isoxazoline ectoparasiticide for dogs." Veterinary Parasitology 222 (2016): 3-11.
[2] Six, Robert H., et al. "Efficacy of sarolaner, a novel oral isoxazoline, against two common mite infestations in dogs: Demodex spp. and Otodectes cynotis." Veterinary Parasitology 222 (2016): 62-66.
[3] Campos, Diefrey R., et al. "Efficacy of oral sarolaner against Lynxacarus radovskyi in naturally infested cats." Veterinary Dermatology 31.5 (2020): 355-e92.
| Animal experiment [1]: | |
Animal models | Beagles dogs |
Preparation Method | On Day-7, each dog was infested with Rhipicephalus sanguineus. On Day-5, the ticks on each dog were counted, dogs were ranked by descending tick count into blocks, and randomly allocated within blocks to two treatment groups of eight dogs each. On Day-2, the dogs were weighed and infested with R. sanguineus and Dermacentor reticulatus ticks. On Day-1, the dogs were infested with fleas. On Day 0, each animal was treated via oral gavage at 0.5mL/kg body weight with either placebo control or sarolaner solution (5mg/mL) to provide a dose of 2.5mg/kg. A tetraglycol/solutol solution base was used to formulate the sarolaner. Dogs were observed for general health and any reaction to treatment approximately 1, 3 and 6h after treatment on Day 0, then once daily for the remainder of the study. On Day 2, each dog was examined and combed to count and remove fleas and ticks. Subsequently, all animals were infested with R. sanguineus and D. reticulatus on Days 5, 12, 19, 25 and 33, and with fleas on Days 6, 13, 20, 26 and 34. All dogs were examined, combed and parasite counted on Days 7, 14, 21, 27 and 35. |
Dosage form | 2.5mg/kg; oral gavage; once |
Applications | Sarolaner was 100% efficacious at 48h after treatment and against subsequent infestations through Day 35. |
References: | |
| Cas No. | 1398609-39-6 | SDF | |
| Synonyms | PF-6450567 | ||
| Canonical SMILES | O=S(CC(N1CC2(OCC3=C2C=CC(C4=NO[C@](C(F)(F)F)(C5=CC(Cl)=C(F)C(Cl)=C5)C4)=C3)C1)=O)(C)=O | ||
| Formula | C23H18Cl2F4N2O5S | M.Wt | 581.36 |
| Solubility | DMSO : 150 mg/mL (258.02 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at 4°C, sealed storage, away from moisture |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7201 mL | 8.6005 mL | 17.201 mL |
| 5 mM | 344 μL | 1.7201 mL | 3.4402 mL |
| 10 mM | 172 μL | 860.1 μL | 1.7201 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)