Setiptiline
Based on 1 Customer Validation
Setiptiline (Org-8282) is a tetracyclic antidepressant and orally active 5-HT1ₑR/5-HT1FR agonist, with an EC50 of 171.0 nM, a Ki of 29.3 nM for human 5-HT1ₑR, and an EC50 of 64.6 nM for human 5-HT1FR. Setiptiline induces the dissociation of G proteins from the heterotrimeric Gαi1/Gβ1/Gγ2 complex and promotes the recruitment of β-arrestin2. Setiptiline is applicable to research related to migraine and schizophrenia.
For research use only. We do not sell to patients.
- Purity : 98.03%
- CAS No.: 57262-94-9
- Formula: C19H19N
- Molecular Weight:261.37
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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
Biological Activity
Description
IC50 & Target
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5-HT3 Receptor |
5-HT2C Receptor |
5-HT2A Receptor |
α adrenergic receptor |
In Vitro
Setiptiline (Serial dilutions; 20 min at 37°C plus 10 min at room temperature) acts as a potent full agonist at human 5-HT1ₑR (EC50 = 171.0 nM) and human 5-HT1F1R (EC50 = 64.6 nM) in a G protein dissociation BRET assay in HEK293T cells[1].
Setiptiline (Serial dilutions; 80 min at room temperature) binds to wild-type human 5-HT1ₑR with a Ki of 29.3 nM in a radioligand competition binding assay[1].
Setiptiline (10 μM; 30 min at room temperature, overnight resin binding) binds to human 5-HT1ₑR in a unique agonist-like pose, forming key interactions with the receptor's orthosteric pocket to stabilize the active-state G protein-coupled complex at 3.32 Å global resolution, as revealed by cryo-EM structural analysis[1].
Setiptiline (Serial dilutions; 20 min at 37°C plus 10 min at room temperature) has increased agonist potency, resulting in greater potency than 5-HT, at human 5-HT1ₑR with the E3116·55D mutation in a G protein dissociation BRET assay in HEK293T cells[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. 57262-94-9
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Appearance Solid
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Molecular Weight 261.37
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Formula C19H19N
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Color White to off-white
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SMILES
CN1CC2=C(CC1)C3=CC=CC=C3CC4=C2C=CC=C4
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Synonyms
Org-8282
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
In Vitro:
DMSO : 25 mg/mL (95.65 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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.
In Vivo Dissolution Calculator
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.
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 (300 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.8260 mL | 19.1300 mL | 38.2599 mL | 95.6498 mL |
| 5 mM | 0.7652 mL | 3.8260 mL | 7.6520 mL | 19.1300 mL | |
| 10 mM | 0.3826 mL | 1.9130 mL | 3.8260 mL | 9.5650 mL | |
| 15 mM | 0.2551 mL | 1.2753 mL | 2.5507 mL | 6.3767 mL | |
| 20 mM | 0.1913 mL | 0.9565 mL | 1.9130 mL | 4.7825 mL | |
| 25 mM | 0.1530 mL | 0.7652 mL | 1.5304 mL | 3.8260 mL | |
| 30 mM | 0.1275 mL | 0.6377 mL | 1.2753 mL | 3.1883 mL | |
| 40 mM | 0.0956 mL | 0.4782 mL | 0.9565 mL | 2.3912 mL | |
| 50 mM | 0.0765 mL | 0.3826 mL | 0.7652 mL | 1.9130 mL | |
| 60 mM | 0.0638 mL | 0.3188 mL | 0.6377 mL | 1.5942 mL | |
| 80 mM | 0.0478 mL | 0.2391 mL | 0.4782 mL | 1.1956 mL |
Setiptiline Related Classifications
HY-32329 Related Classifications
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