| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 2mg | |||
| 5mg | |||
| Other Sizes |
| Targets |
Ziprasidone D8 targets the same receptors as the unlabeled compound ziprasidone, which is a combined serotonin (5-HT2A) and dopamine (D2) receptor antagonist. It binds to 5-HT₂A and dopamine D₂ receptors with Ki values of 1.15 and 1.29 nM, respectively. The compound exhibits potent antipsychotic activity by blocking these receptors, which are involved in the pathophysiology of schizophrenia and bipolar disorder.
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|---|---|
| ln Vitro |
In vitro, ziprasidone D8 serves as an analytical standard rather than being directly tested for receptor binding. The unlabeled compound ziprasidone is a potent antagonist at 5-HT₂A and dopamine D₂ receptors with Ki values of 1.15 and 1.29 nM, respectively. It also shows activity at other serotonin and dopamine receptor subtypes. The compound is an atypical antipsychotic with a unique mechanism of action that distinguishes it from other antipsychotic drugs.
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| ln Vivo |
In vivo, ziprasidone D8 is used as an internal standard in pharmacokinetic studies rather than being administered as a therapeutic agent. The unlabeled compound ziprasidone is an approved atypical antipsychotic for the treatment of schizophrenia and bipolar disorder. Ziprasidone inhibits d-amphetamine-induced hyperactivity and apomorphine-induced stereotypy in rats with ID₅₀ values of 1.53 and 2.43 mg/kg, respectively, confirming its in vivo antipsychotic activity.
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| Enzyme Assay |
For non-cell enzyme/receptor binding assays, ziprasidone D8 is used as an internal standard in analytical method development. The compound is characterized by detailed analytical data including NMR, HPLC, and GC. It is used in method validation and quality control applications for ziprasidone production. The deuterated compound co-elutes with unlabeled ziprasidone in chromatographic methods but is distinguished by mass spectrometry due to the mass shift.
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| Cell Assay |
For in vitro cell-based assays, ziprasidone D8 is typically not used for receptor binding studies. Instead, it serves as an analytical standard in cell culture studies where ziprasidone concentrations need to be quantified. The deuterated compound is added to cell culture samples as an internal standard before extraction and LC-MS/MS analysis to accurately determine the concentration of unlabeled ziprasidone in the samples.
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| Animal Protocol |
For in vivo animal experiments, ziprasidone D8 is used as an internal standard in pharmacokinetic studies. Animals are administered unlabeled ziprasidone, and blood or tissue samples are collected. Ziprasidone D8 is added to the samples as an internal standard before sample preparation and LC-MS/MS analysis. This allows accurate quantification of ziprasidone concentrations in biological matrices, enabling the determination of pharmacokinetic parameters. The recovery rate for Ziprasidone D8 from biological matrices is 95.70%.
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| ADME/Pharmacokinetics |
Ziprasidone D8 has a molecular weight of 421.0 g/mol and molecular formula C₂₁H₁₃D₈ClN₄OS. The compound is supplied with high purity (≥98%) and detailed characterization data compliant with regulatory guidelines. It is a stable isotope-labeled compound used for analytical method development, method validation, and quality control applications. The compound should be stored under recommended conditions for long-term stability.
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| Toxicity/Toxicokinetics |
Ziprasidone D8 is a deuterated compound used for research and analytical applications only. It is not intended for human therapeutic use. The toxicity profile is similar to that of unlabeled ziprasidone, which is generally well-tolerated at therapeutic doses. Standard safety precautions for handling research chemicals should be followed. The compound is not approved as a therapeutic agent in its labeled form.
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| Additional Infomation |
Ziprasidone D8 is a stable isotope-labeled internal standard used in the pharmaceutical industry for analytical method development and quality control of ziprasidone, an FDA-approved atypical antipsychotic for the treatment of schizophrenia and bipolar disorder. The compound can be used for Abbreviated New Drug Application (ANDA) submissions and during commercial production of ziprasidone. It is not a therapeutic agent itself but a crucial tool for accurate drug quantification in pharmacokinetic and bioanalytical studies.
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| Molecular Formula |
C21H13D8N4OSCL
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|---|---|
| Molecular Weight |
420.985
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| Exact Mass |
420.162
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| CAS # |
1126745-58-1
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| Related CAS # |
Ziprasidone;146939-27-7;Ziprasidone hydrochloride monohydrate;138982-67-9;Ziprasidone hydrochloride;122883-93-6;Ziprasidone mesylate trihydrate;199191-69-0;Ziprasidone mesylate;185021-64-1
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| PubChem CID |
25216238
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| Appearance |
Light yellow to khaki solid powder
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| LogP |
3.949
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
573
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C1(C(N(C(C(N1CCC2=C(C=C3C(=C2)CC(=O)N3)Cl)([2H])[2H])([2H])[2H])C4=NSC5=CC=CC=C54)([2H])[2H])[2H]
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| InChi Key |
MVWVFYHBGMAFLY-UFBJYANTSA-N
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| InChi Code |
InChI=1S/C21H21ClN4OS/c22-17-13-18-15(12-20(27)23-18)11-14(17)5-6-25-7-9-26(10-8-25)21-16-3-1-2-4-19(16)28-24-21/h1-4,11,13H,5-10,12H2,(H,23,27)/i7D2,8D2,9D2,10D2
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| Chemical Name |
5-[2-[4-(1,2-benzothiazol-3-yl)-2,2,3,3,5,5,6,6-octadeuteriopiperazin-1-yl]ethyl]-6-chloro-1,3-dihydroindol-2-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 | 2.3754 mL | 11.8768 mL | 23.7535 mL | |
| 5 mM | 0.4751 mL | 2.3754 mL | 4.7507 mL | |
| 10 mM | 0.2375 mL | 1.1877 mL | 2.3754 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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