Octoclothepine
Based on 1 publication(s) in Google Scholar
Octoclothepin (Clorotepine) is a D2 dopamine receptor antagonist and 5-HT2 serotonin receptor antagonist , with Ki values of 0.67 nM, 0.57 nM, and 0.19 nM for the dopamine D2, 5-HT2A, and 5-HT2C receptors, respectively. Octoclothepin also binds to adrenergic receptors, with Ki values of 0.66 nM, 0.56 nM, and 0.77 nM for α1a, α1b, and α1d, respectively. Octoclothepin can be used in schizophrenia research.
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 13448-22-1
- Formula: C19H21ClN2S
- Molecular Weight:344.90
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Octoclothepine
MoreAll 5-HT Receptor Isoforms
More
Biological Activity
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5-HT6 Receptor |
5-HT7 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
73.8 μM
Compound: Octoclothepin
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Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay
Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay
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[PMID: 31260312] |
Octoclothepin (Compound 8) binds with subnanomolar to nanomolar affinity to bovine α1a-, hamster α1b-, rat α1d-adrenoceptors, human D2, human 5-HT2A, and human 5-HT2C receptors, , with Ki values of 0.66 nM, 0.56 nM, 0.77 nM, 0.67 nM, 0.57 nM, and 0.19 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 13448-22-1
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Appearance Solid
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Molecular Weight 344.90
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Formula C19H21ClN2S
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Color White to off-white
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SMILES
CN1CCN(C2CC3=CC=CC=C3SC4=CC=C(Cl)C=C24)CC1
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Synonyms
Clorotepine
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
A drug repurposing screen reveals dopamine signaling as a candidate therapeutic pathway for PIGA-CDG. [Abstract]2026 Apr 18:2026.04.17.719256. PMID: 42039650
Solvent & Solubility
DMSO : 10 mg/mL (28.99 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.90 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1].
Helia O, et al. Reduction of octoclothepine-N-oxide by rat liver microsomes. Eur J Drug Metab Pharmacokinet. 1981;6(2):155-8.
[Content Brief]
[2].
Roth BL, et al. Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J Pharmacol Exp Ther. 1994 Mar;268(3):1403-10.
[Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8994 mL | 14.4970 mL | 28.9939 mL | 72.4848 mL |
| 5 mM | 0.5799 mL | 2.8994 mL | 5.7988 mL | 14.4970 mL | |
| 10 mM | 0.2899 mL | 1.4497 mL | 2.8994 mL | 7.2485 mL | |
| 15 mM | 0.1933 mL | 0.9665 mL | 1.9329 mL | 4.8323 mL | |
| 20 mM | 0.1450 mL | 0.7248 mL | 1.4497 mL | 3.6242 mL | |
| 25 mM | 0.1160 mL | 0.5799 mL | 1.1598 mL | 2.8994 mL |
Octoclothepine Related Classifications
HY-106587 Related Classifications
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- Octoclothepine
- 13448-22-1
- Clorotepine
- 5-HT Receptor
- Drug Derivative
- serotonin 5-HT2C receptors
- α1-adrenoceptor subtypes
- dopamine D2 receptors
- rat α1d-adrenoceptors
- serotonin 5-HT2A receptors
- bovine α1a-adrenoceptors
- human H1 receptors
- human D2 receptors
- histamine H1 receptors
- hamster α1b-adrenoceptors
- Inhibitor
- inhibitor
- inhibit