SB 271046 Hydrochloride
Based on 1 Customer Validation
SB 271046 Hydrochloride (SB 271046A) is a potent, selective, orally active and BBB-permeable 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM).
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 209481-24-3
- Formula: C20H23Cl2N3O3S2
- Molecular Weight:488.45
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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All 5-HT Receptor Isoforms
More
Biological Activity
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5-HT6 Receptor 8.92-9.02 (pKi) |
5-HT6 Receptor |
5-HT1D Receptor 6.55 (pKi) |
5-HT1A Receptor 6.35 (pKi) |
5-HT1B Receptor 6.05 (pKi) |
5-HT1F Receptor 5.95 (pKi) |
5-HT2A Receptor 5.62 (pKi) |
5-HT2B Receptor 5.41 (pKi) |
5-HT7 Receptor 5.39 (pKi) |
5-HT4 Receptor 5.27 (pKi) |
5-HT1E Receptor <4.99 (pKi) |
Human 5-HT2C Receptor 5.73 (pKi) |
SB 271046 Hydrochloride (SB 271046A) shows pKi values of 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively. SB-271046 Hydrochloride competitively antagonizes 5-HT-induced stimulation of adenylyl cyclase activity with a pA2 of 8.71[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague Dawley rats[1]
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Dosage:10 mg/kg
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Administration:P.o.
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Result:Produced an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of ⩽0.1 mg kg−1 p.o. and maximum effect at 4 h post-dose. The level of anticonvulsant activity achieved correlated well with the blood concentrations of SB-271046 (EC50 of 0.16 μM) and brain concentrations of 0.01-0.04 μM at Cmax.
Chemical Information
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CAS No. 209481-24-3
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Appearance Solid
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Molecular Weight 488.45
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Formula C20H23Cl2N3O3S2
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Color White to light brown
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SMILES
ClC1=CC2=C(C=C1)SC(S(=O)(NC3=CC=C(C(N4CCNCC4)=C3)OC)=O)=C2C.[H]Cl
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Synonyms
SB 271046A
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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
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 50 mg/mL (102.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 1 mg/mL (2.05 mM; ultrasonic and warming and heat to 60°C)
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 2.5 mg/mL (5.12 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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)
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 (273 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.0473 mL | 10.2365 mL | 20.4729 mL | 51.1823 mL |
| DMSO | 5 mM | 0.4095 mL | 2.0473 mL | 4.0946 mL | 10.2365 mL |
| 10 mM | 0.2047 mL | 1.0236 mL | 2.0473 mL | 5.1182 mL | |
| 15 mM | 0.1365 mL | 0.6824 mL | 1.3649 mL | 3.4122 mL | |
| 20 mM | 0.1024 mL | 0.5118 mL | 1.0236 mL | 2.5591 mL | |
| 25 mM | 0.0819 mL | 0.4095 mL | 0.8189 mL | 2.0473 mL | |
| 30 mM | 0.0682 mL | 0.3412 mL | 0.6824 mL | 1.7061 mL | |
| 40 mM | 0.0512 mL | 0.2559 mL | 0.5118 mL | 1.2796 mL | |
| 50 mM | 0.0409 mL | 0.2047 mL | 0.4095 mL | 1.0236 mL | |
| 60 mM | 0.0341 mL | 0.1706 mL | 0.3412 mL | 0.8530 mL | |
| 80 mM | 0.0256 mL | 0.1280 mL | 0.2559 mL | 0.6398 mL | |
| 100 mM | 0.0205 mL | 0.1024 mL | 0.2047 mL | 0.5118 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
SB 271046 Hydrochloride Related Classifications
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