| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
Purity: ≥98%
Sarolaner (also known as PF-6450567; PF6450567) is a novel, potent, orally bioactive and broad-spectrum ectoparasiticide (an antiparasitic agent for veterinary use). It has efficacy against fleas and ticks on dogs with LC80 of 0.3 μg/mL against C. felis and an LC100 of 0.003 μg/mL against O. turicata.
| ln Vitro |
Sarolaner (450 nM-1 mM; 5 minutes) suppresses currents produced by gamma-buffered butyric acid (GABA) on CfRDL-A285 and CfRDL-S285 receptors [1].
|
|---|---|
| ln Vivo |
Sarolaner shown 100% effectiveness against R at 2.5 mg/kg; main sidewall. sanguineus as well as D. reticuLatus [1]. Sarolaner, which acts against I, is efficacious at 1.25–5 mg/kg (primary sidewall). ricinus [1].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: CHO-K1 Cell Tested Concentrations: 450 nM-1 mM Incubation Duration: 5 minutes Experimental Results: Inhibition of GABA-elicited current of susceptible fleas (CfRDL-A285) and resistant fleas GABACl, EC50 is 135 respectively and 136 nM. |
| Animal Protocol |
Animal/Disease Models: Dogs infected with R. sanguineus and D. reticulatus [1]
Doses: 2.5 mg/kg Route of Administration: po (oral gavage); 2.5 mg/kg One time Experimental Results:100% efficacy against R. sanguineus 48 hrs (hrs (hours)) after treatment , also has 98.0% efficacy against D. d. Net pattern. Animal/Disease Models: Ricin-infected dogs [1] Doses: 1.25, 2.5 and 5 mg/kg Route of Administration: po (oral gavage); 1.25, 2.5 and 5 mg/kg Primary Experimental Results: Prior to 7 days, all doses were effective in ricin Both narcotics demonstrated 100% efficacy and diminished subsequent reinfections by more than 99.3% by 57 days at doses of 5.0 and 2.5 mg/kg. |
| References | |
| Additional Infomation |
See also: Moxidectin; Pyrantel Pamoate; Sarolaner (component of); Sarolaner; Selamectin (component of).
Drug Indication For the treatment of tick infestations (Dermacentor reticulatus, Ixodes hexagonus, Ixodes ricinus and Rhipicephalus sanguineus). The veterinary medicinal product has immediate and persistent tick killing activity for at least 5 weeks. For the treatment of flea infestations (Ctenocephalides felis and Ctenocephalides canis). The veterinary medicinal product has immediate and persistent flea killing activity against new infestations for at least 5 weeks. The veterinary medicinal product can be used as part of a treatment strategy for the control of Flea Allergy Dermatitis (FAD). For the treatment of sarcoptic mange (Sarcoptes scabiei). For the treatment of ear mite infestations (Otodectes cynotis). For the treatment of demodicosis (Demodex canis). Fleas and ticks must attach to the host and commence feeding in order to be exposed to the active substance. For the treatment of tick infestations (Dermacentor reticulatus, Ixodes hexagonus,Ixodes ricinus and Rhipicephalus sanguineus). The veterinary medicinal product has immediate and persistent tick killing activity for at least 5 weeks. , , For the treatment of flea infestations (Ctenocephalides felis and Ctenocephalides canis). The veterinary medicinal product has immediate and persistent flea killing activity against new infestations for at least 5 weeks. The veterinary medicinal product can be used as part of a treatment strategy for the control of Flea Allergy Dermatitis (FAD). , , For the treatment of sarcoptic mange (Sarcoptes scabiei). , , For the treatment of ear mite infestations (Otodectes cynotis). , , For the treatment of demodicosis (Demodex canis). , , Fleas and ticks must attach to the host and commence feeding in order to be exposed to the active substance. , |
| Molecular Formula |
C23H18CL2F4N2O5S
|
|---|---|
| Molecular Weight |
581.364037036896
|
| Exact Mass |
580.025
|
| CAS # |
1398609-39-6
|
| PubChem CID |
73169092
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.781
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
37
|
| Complexity |
1050
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CS(=O)(=O)CC(=O)N1CC2(C1)C3=C(CO2)C=C(C=C3)C4=NO[C@@](C4)(C5=CC(=C(C(=C5)Cl)F)Cl)C(F)(F)F
|
| InChi Key |
FLEFKKUZMDEUIP-QFIPXVFZSA-N
|
| InChi Code |
InChI=1S/C23H18Cl2F4N2O5S/c1-37(33,34)9-19(32)31-10-21(11-31)15-3-2-12(4-13(15)8-35-21)18-7-22(36-30-18,23(27,28)29)14-5-16(24)20(26)17(25)6-14/h2-6H,7-11H2,1H3/t22-/m0/s1
|
| Chemical Name |
(S)-1-(5'-(5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-3'H-spiro[azetidine-3,1'-isobenzofuran]-1-yl)-2-(methylsulfonyl)ethan-1-one
|
| Synonyms |
PF6450567; PF 6450567; PF-6450567
|
| 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: Please store this product in a sealed and protected environment, 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)
|
| Solubility (In Vitro) |
DMSO : ~300 mg/mL (~516.03 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 7.5 mg/mL (12.90 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 75.0 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: ≥ 7.5 mg/mL (12.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 75.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7201 mL | 8.6005 mL | 17.2010 mL | |
| 5 mM | 0.3440 mL | 1.7201 mL | 3.4402 mL | |
| 10 mM | 0.1720 mL | 0.8601 mL | 1.7201 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA