| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Coccidia
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|---|---|
| ln Vitro |
Toltrazuril sulfone prevents S. neurona merozoite development[1].
48 hours after exposure, toltrazuril sulfone inhibits the growth of N. caninum[1].
Toltrazuril sulfone may have inhibitory effects on various apicomplexans by targeting distinct enzymes or enzyme systems[1].
Following the second division by endodyogeny, toltrazuril sulfone (5 mg/ml; 20 hours) inhibits T. gondii replication[2].
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| ln Vivo |
For ten days, toltrazuril sulfone (10–20 mg/kg; p.o.) is an effective treatment for both prevention and treatment of toxoplasmosis in mice[2].
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| Animal Protocol |
Animal Model: Female CD-1 mice[2]
Dosage: 10 mg/kg, 20 mg/kg Administration: Oral administration, daily, for 10 days Result: Prevented and protected mice from toxoplasmosis. The in vivo efficacy of Ponazuril was tested in outbred female CD-1 mice. A suspension of Ponazuril (50 mg/ml) was diluted in distilled water and administered orally. All mice were infected subcutaneously in the dorsal scapular region with 1 × 10³ tachyzoites of the RH strain of *T. gondii*. [2] For the prevention study, mice (5 per group) were treated daily for 10 days with 10 or 20 mg/kg Ponazuril, starting one day before infection. For the treatment study, mice (5 per group) were treated daily for 10 days with 10, 20, or 50 mg/kg Ponazuril, starting 3 or 6 days after infection. Control groups received distilled water. Mice were weighed daily and monitored for mortality. At 8 weeks post-infection, surviving mice were bled, and serum was tested for antibodies to *T. gondii* using a modified direct agglutination test (MAT). Brains were collected for PCR analysis to detect *T. gondii* DNA. [2] |
| References | |
| Additional Infomation |
Ponazuril, sold by Bayer under the brand name Marquis, is a drug currently approved for the treatment of equine protozoan spinal encephalitis caused by Sarcocystis neurona.
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| Exact Mass |
457.056
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|---|---|
| Elemental Analysis |
C, 47.27; H, 3.09; F, 12.46; N, 9.19; O, 20.99; S, 7.01
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| CAS # |
69004-04-2
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| Related CAS # |
Toltrazuril;69004-03-1
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| PubChem CID |
3050408
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| Appearance |
Solid powder
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| Density |
1.507g/cm3
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| Melting Point |
242°
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| Index of Refraction |
1.572
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| LogP |
2.699
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
836
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VBUNOIXRZNJNAD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H14F3N3O6S/c1-10-9-11(24-16(26)22-15(25)23(2)17(24)27)3-8-14(10)30-12-4-6-13(7-5-12)31(28,29)18(19,20)21/h3-9H,1-2H3,(H,22,25,26)
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| Chemical Name |
1-Methyl-3-(4-(p-((trifluoromethyl)sulfonyl)phenoxy)-m-tolyl)-s-triazine-2,4,6(1H,3H,5H)-trione.
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| Synonyms |
BAY-Vi 9143; BAY-Vi-9143; BAY-Vi9143; Ponazuril; Toltrazuril sulfone; Marquis.
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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 |
| 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 : ~50 mg/mL (~109.32 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.47 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 25.0 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: ≥ 2.5 mg/mL (5.47 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00270933 | COMPLETED | Device: Registry | Ventricular Fibrillation Ventricular Tachycardia |
Medtronic Cardiac Rhythm and Heart Failure | 2004-01 | |
| NCT00271232 | COMPLETED | Device: Cardiac resynchronization therapy |
Heart Failure | Medtronic Cardiac Rhythm and Heart Failure | 2003-03 | Not Applicable |
| NCT00157820 | COMPLETEDWITH RESULTS | Device: Single Chamber Implantable Cardioverter Defibrillator Device: Dual Chamber implantable cardioverter defibrilator |
Defibrillators, Implantable Ventricular Fibrillation Ventricular Tachycardia |
Medtronic Bakken Research Center | 2000-11 | Not Applicable |
| NCT01337063 | COMPLETED | Other: Mentored medication reconciliation quality improvement |
Adverse Drug Events Medication Administered in Error |
Brigham and Women's Hospital | 2011-03 | Not Applicable |
| NCT00170313 | TERMINATED | Device: Conducted AF-Response Algorithm (CAFR) On Device: Conducted AF-Response Algorithm (CAFR) Off |
Atrial Fibrillation Heart Failure Sudden Cardiac Death |
Medtronic Bakken Research Center | 2003-12 | Phase 4 |