| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Schistosomes and other flatworms (anthelmintic). Praziquantel is the active anthelmintic agent that increases the permeability of trematode and cestode cell membranes to calcium ions, causing strong contraction and paralysis of the worm's musculature, leading to detachment from host tissues and subsequent death.
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| ln Vitro |
(S)-Praziquantel-d11 itself is not assessed for biological activity in the same way as a drug candidate. The non-deuterated praziquantel is a broad-spectrum anthelmintic drug with potent activity against Schistosoma species (MICs in the low microg/mL range). In vitro, praziquantel induces rapid contraction and tegumental damage in adult schistosomes, leading to parasite death. The (S)-enantiomer is the more active stereoisomer compared to the (R)-enantiomer.
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| ln Vivo |
No pharmacological activity data is provided for (S)-Praziquantel-d11 itself. The non-deuterated praziquantel is clinically used as an anthelmintic. In animal models of schistosomiasis, praziquantel effectively reduces worm burden and egg production. In infected rodents, oral administration of praziquantel (100-500 mg/kg) results in significant reduction of Schistosoma mansoni, S. haematobium, and S. japonicum worm loads.
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| Enzyme Assay |
For enzyme inhibition assays, since (S)-Praziquantel-d11 is an internal standard, its primary use is in analytical chemistry rather than binding assays. A radioligand binding assay for the parent drug would use membrane preparations from schistosomes incubated with [3H]-praziquantel in assay buffer. After incubation at 25degC for 60 minutes, bound and free radioligand are separated by filtration, and radioactivity is counted to determine binding parameters.
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| Cell Assay |
A standard method involves spiking a known amount of the deuterated internal standard into biological samples. After protein precipitation or solid-phase extraction, the supernatant is injected onto a LC-MS/MS system with a C18 column. The deuterated internal standard and the non-deuterated analyte are detected in multiple reaction monitoring mode, and peak area ratios are used for quantification. Standard curves are prepared in blank matrix.
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| Animal Protocol |
For in vivo pharmacokinetic studies, the internal standard is not administered directly. The non-deuterated praziquantel is typically administered orally to rats or dogs at doses of 10-50 mg/kg. Blood samples are collected at predetermined time points (e.g., 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 12, 24 hours). Plasma is separated, and the internal standard is added to each sample before LC-MS/MS analysis. PK parameters including Cmax, Tmax, AUC, t1/2, and bioavailability are calculated.
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| ADME/Pharmacokinetics |
(S)-Praziquantel-d11 itself has no PK properties. For the parent compound praziquantel, pharmacokinetic parameters include oral bioavailability of approximately 80%, extensive distribution (Vd = 1-2 L/kg), high plasma protein binding (80%), and a terminal half-life (t1/2) of 1-3 hours in humans. The drug is extensively metabolized in the liver, primarily by CYP3A4, to inactive hydroxylated metabolites, which are excreted in urine.
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| Toxicity/Toxicokinetics |
As a deuterated internal standard, (S)-Praziquantel-d11 is not intended for therapeutic use. The parent compound praziquantel is clinically approved and has a well-established safety profile. Side effects are generally mild and transient, including headache, dizziness, abdominal pain, and nausea. Praziquantel is contraindicated in ocular cysticercosis and should be used with caution in patients with liver disease. No genotoxicity or carcinogenicity has been reported.
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| References | |
| Additional Infomation |
(S)-Praziquantel-d11 is a research-grade chemical used as an internal standard for LC-MS/MS quantification in pharmacokinetic, bioavailability, and bioequivalence studies of praziquantel-containing formulations. Praziquantel is a World Health Organization (WHO) essential medicine for the treatment of schistosomiasis. The WHO recommends mass drug administration (MDA) with praziquantel to control schistosomiasis in endemic regions. This product is for research use only and is not FDA-approved.
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| Molecular Formula |
C19H13D11N2O2
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|---|---|
| Molecular Weight |
323.47
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| Appearance |
White to off-white solid powder
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.0915 mL | 15.4574 mL | 30.9148 mL | |
| 5 mM | 0.6183 mL | 3.0915 mL | 6.1830 mL | |
| 10 mM | 0.3091 mL | 1.5457 mL | 3.0915 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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