| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
(R)-Praziquantel D11 targets the same receptors as Praziquantel. Praziquantel is a partial agonist of the human 5-HT2B receptor. It is used as an anthelmintic drug for the treatment of schistosomiasis and other parasitic worm infections. The deuterium labeling does not significantly alter receptor binding affinity or selectivity, but provides a mass shift that allows differentiation from the unlabeled compound in analytical assays.
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| ln Vitro |
(R)-Praziquantel ((R)-PZQ) is a receptor ligand linked to G proteins. Within a concentration range that is adequate to alter vascular tone in the mesenteric arteries of the adult worm living in its host, (R)-praziquantel modulates serotonergic signaling. Extensive cross-species polypharmacology supports the effectiveness of this significant anthelmintic, since (R)-praziquantel modulates host and parasite signaling processes [1].
In vitro studies with (R)-Praziquantel D11 primarily focus on its use as an analytical internal standard rather than its pharmacological activity. The compound is used in LC-MS/MS methods for the quantification of Praziquantel in biological matrices. The deuterium labeling provides a mass shift that allows differentiation from the unlabeled compound, enabling accurate quantification. The compound's in vitro activity at the 5-HT2B receptor is expected to be similar to that of unlabeled (R)-Praziquantel. |
| ln Vivo |
In vivo studies using (R)-Praziquantel D11 are primarily pharmacokinetic, where the compound serves as an internal standard for the quantification of Praziquantel in biological samples. The deuterium-labeled compound can be co-administered with unlabeled Praziquantel to study absorption, distribution, metabolism, and excretion. It has been used in bioequivalence studies and method validation for regulatory submissions. Its in vivo pharmacological effects are expected to be similar to those of Praziquantel, a drug used to treat schistosomiasis and other parasitic worm infections.
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| Enzyme Assay |
In vitro enzyme/receptor binding (non-cell) assays for (R)-Praziquantel D11 are typically performed as part of analytical method validation rather than pharmacological characterization. The compound is used as an internal standard in LC-MS/MS assays for the quantification of Praziquantel. Receptor binding assays (e.g., 5-HT2B binding) can be performed using membrane preparations and radioligand binding, but the deuterated compound is primarily used for analytical purposes. The compound is dissolved in appropriate solvents (methanol, acetonitrile, or DMSO) and spiked into biological matrices at known concentrations. Calibration curves are generated by plotting the peak area ratio of Praziquantel to (R)-Praziquantel D11 against the concentration of Praziquantel.
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| Cell Assay |
For in vitro cell-based assays, (R)-Praziquantel D11 can be used in studies investigating Praziquantel's cellular effects. Cells expressing 5-HT2B receptors are cultured in appropriate media and treated with the compound. Receptor activation is measured by quantifying intracellular calcium mobilization or other downstream signaling pathways. However, the compound's primary use is as an analytical internal standard. Cell viability and cytotoxicity are assessed using MTT or CCK-8 assays. The compound's cellular effects are expected to be similar to those of unlabeled Praziquantel.
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| Animal Protocol |
In vivo animal studies with (R)-Praziquantel D11 are primarily pharmacokinetic. The compound is administered orally or intravenously to rodents at doses determined from pharmacokinetic studies, and blood samples are collected at predetermined time points. Plasma concentrations of both labeled and unlabeled Praziquantel are analyzed by LC-MS/MS using (R)-Praziquantel D11 as the internal standard. For pharmacodynamic studies, the compound's effects on parasitic worm infections can be evaluated in appropriate animal models. The deuterium labeling may affect the compound's metabolic stability, potentially altering its pharmacokinetic profile.
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| ADME/Pharmacokinetics |
(R)-Praziquantel D11 has a molecular weight of 323.47 g/mol and molecular formula C19H13D11N2O2. The compound is a deuterium-labeled analog of the active enantiomer of Praziquantel. Pharmacokinetic properties are expected to be similar to Praziquantel, with the deuterium labeling potentially altering metabolic stability due to the isotope effect. Praziquantel is rapidly absorbed after oral administration and undergoes extensive first-pass metabolism. The compound is primarily excreted via urine. (R)-Praziquantel D11 is used in very small quantities as an analytical internal standard.
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| Toxicity/Toxicokinetics |
As a deuterium-labeled analogue of an approved drug, (R)-Praziquantel D11 is expected to have a similar toxicity profile to Praziquantel, though toxicity studies are typically not performed on the labeled compound due to its use as an analytical standard. Praziquantel is generally well-tolerated with common side effects including headache, dizziness, and gastrointestinal disturbances. (R)-Praziquantel D11 is used in very small quantities as an analytical internal standard and does not pose significant toxicity risks under normal handling.
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| References | |
| Additional Infomation |
(R)-Praziquantel D11 is a deuterium-labeled form of (R)-Praziquantel, the active enantiomer of Praziquantel. Praziquantel is a partial agonist of the human 5-HT2B receptor and is used as an anthelmintic drug for the treatment of schistosomiasis and other parasitic worm infections. (R)-Praziquantel D11 is used as an internal standard for analytical method development, method validation, and pharmacokinetic studies. The compound is intended for research and analytical use only, not for human or clinical use.
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| Molecular Formula |
C19H24N2O2
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|---|---|
| Molecular Weight |
312.406064987183
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| Exact Mass |
323.252
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| CAS # |
1399880-38-6
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| PubChem CID |
89398666
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| Appearance |
White to off-white solid powder
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| LogP |
2.7
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
23
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| Complexity |
472
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O=C1CN(C(C2([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C2([H])[H])=O)C[C@@]2([H])C3=CC=CC=C3CCN12
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| InChi Key |
FSVJFNAIGNNGKK-OABFBXGMSA-N
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| InChi Code |
InChI=1S/C19H24N2O2/c22-18-13-20(19(23)15-7-2-1-3-8-15)12-17-16-9-5-4-6-14(16)10-11-21(17)18/h4-6,9,15,17H,1-3,7-8,10-13H2/t17-/m0/s1/i1D2,2D2,3D2,7D2,8D2,15D
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| Chemical Name |
(11bR)-2-(1,2,2,3,3,4,4,5,5,6,6-undecadeuteriocyclohexanecarbonyl)-3,6,7,11b-tetrahydro-1H-pyrazino[2,1-a]isoquinolin-4-one
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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 | 3.2009 mL | 16.0046 mL | 32.0092 mL | |
| 5 mM | 0.6402 mL | 3.2009 mL | 6.4018 mL | |
| 10 mM | 0.3201 mL | 1.6005 mL | 3.2009 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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