| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Clothiapine targets serotonin 5-HT2 receptors and dopamine D2 receptors. It exhibits strong affinity for 5-HT2 receptors and moderate affinity for D2 receptors. The compound is also described as a serotonin 3 (5-HT3) receptor antagonist. By blocking these receptors, Clothiapine modulates serotonergic and dopaminergic neurotransmission, which is the basis for its antipsychotic and anxiolytic effects.
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| ln Vitro |
In vitro, Clothiapine acts as a potent antagonist at serotonin 5-HT2 receptors and dopamine D2 receptors. It also functions as a 5-HT3 receptor antagonist. The compound's strong antiserotonergic properties are shared with clozapine. Its activity is typically assessed in receptor binding assays measuring affinity for 5-HT2 and D2 receptors, as well as in functional assays evaluating receptor-mediated signaling inhibition.
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| ln Vivo |
No specific in vivo activity data is publicly available for Clothiapine beyond its classification as an atypical antipsychotic. It has been investigated for the treatment of schizophrenia and other psychiatric disorders. The compound is not widely marketed but serves as a valuable pharmacological tool for studying serotonergic and dopaminergic neurotransmission.
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| Enzyme Assay |
In cell-free receptor binding assays, Clothiapine's activity is evaluated by measuring its affinity for 5-HT2 and dopamine D2 receptors. Membrane preparations from cells expressing these receptors are incubated with radiolabeled ligands (e.g., [3H]ketanserin for 5-HT2, [3H]spiperone for D2) and varying concentrations of Clothiapine. The displacement of the radioligands is measured, and the Ki values are calculated from competition curves.
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| Cell Assay |
In vitro cell-based experiments with Clothiapine typically involve cell lines expressing 5-HT2 or D2 receptors. Cells are treated with the compound, and receptor activation is assessed by measuring downstream signaling events such as calcium mobilization or cAMP accumulation. The compound's ability to inhibit agonist-induced responses is measured to determine its antagonist potency at each receptor subtype.
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| Animal Protocol |
No specific in vivo animal protocols are publicly available for Clothiapine. If in vivo studies were to be conducted, typical protocols might involve rodent models of schizophrenia (e.g., amphetamine-induced hyperlocomotion, prepulse inhibition) or depression, where the compound would be administered, and behavioral outcomes would be measured.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is publicly available for Clothiapine. As an atypical antipsychotic, it is expected to be orally active and to penetrate the blood-brain barrier to exert its central effects. Its half-life, bioavailability, and metabolism have not been extensively characterized in the available literature.
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| Toxicity/Toxicokinetics |
No specific toxicity data is publicly available for Clothiapine. As an antipsychotic agent, its safety profile would be expected to include potential side effects such as sedation, weight gain, and metabolic changes, similar to other atypical antipsychotics. The compound is for research use only and is not intended for human therapeutic applications.
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| References | |
| Additional Infomation |
Clotiapine is a dibenzothiazole drug. It has been approved in European countries and is an atypical antipsychotic that has been shown to be effective for some patients with treatment-resistant psychosis.
Clothiapine has a molecular formula of C18H18ClN3S and a molecular weight of 343.87. It is also known as HF 2159. The compound is a dibenzothiazepine-class atypical antipsychotic structurally analogous to quetiapine and clozapine. It has been investigated for schizophrenia and other psychiatric disorders but is not widely marketed. It serves as a valuable pharmacological tool for studying serotonergic and dopaminergic neurotransmission. |
| Molecular Formula |
C18H18CLN3S
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|---|---|
| Molecular Weight |
343.873
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| Exact Mass |
343.091
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| CAS # |
2058-52-8
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| PubChem CID |
16351
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| Appearance |
White to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
483.8±55.0 °C at 760 mmHg
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| Melting Point |
121-123℃
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| Flash Point |
246.4±31.5 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.691
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| LogP |
3.13
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
23
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| Complexity |
450
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KAAZGXDPUNNEFN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H18ClN3S/c1-21-8-10-22(11-9-21)18-14-12-13(19)6-7-16(14)23-17-5-3-2-4-15(17)20-18/h2-7,12H,8-11H2,1H3
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| Chemical Name |
8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzothiazepine
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| Synonyms |
HF-2159; HF 2159; Clothiapine
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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 : ~62.5 mg/mL (~181.75 mM)
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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 | 2.9081 mL | 14.5404 mL | 29.0808 mL | |
| 5 mM | 0.5816 mL | 2.9081 mL | 5.8162 mL | |
| 10 mM | 0.2908 mL | 1.4540 mL | 2.9081 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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