2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. SB357134

SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist. SB-357134 enhances memory and learning and increases seizure threshold in rats.

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SB357134

SB357134 Chemical Structure

CAS No. : 219963-52-7

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SB357134 Related Antibodies

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5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

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  • Purity & Documentation

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Description

SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist. SB-357134 enhances memory and learning and increases seizure threshold in rats[1].

IC50 & Target

5-HT6 Receptor

 

In Vitro

SB-357134 (0.1, 0.3, 1, and 3 μM) concentration-dependently inhibits the 5-HT-mediated increased level of cAMP, which is surmountable at high 5-HT concentrations, consistent with competitive antagonism[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SB357134 Related Antibodies
In Vivo

SB-357134 dose-dependently inhibits the specific [125I]SB-258585 binding[1].
SB-357134 (0.03-30 mg/kg; 0-24 h; p.o.; single dose) produces a potent and dose-related anticonvulsant effect in the rat MEST model, with a minimum significantly effective dose of 0.1 mg/kg[1].
Chronic administration of SB-357134 (10 mg/kg; p.o.; twice daily; 7 days) significantly shortens path length compared to vehicle and acute administration of SB-357134[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague–Dawley rats[1]
Dosage: 0.03–30 mg/kg
Administration: 0-24 h; p.o.; 0.03–30 mg/kg
Result: Produced a potent and dose-related anticonvulsant effect in the rat MEST model, with a minimum significantly effective dose of 0.1 mg/kg. Increased seizure threshold up to 123±12% at the highest dose tested of 30 mg/kg. At 10 mg/kg, exhibited a rapid onset of action, significantly increasing seizure threshold from a control value of 21.7 to 26.7 mA at 1 h postdose. Observed Peak activity within 4–6 h postdose. With the exception of an unexplained loss of activity at 12 h, had a long duration of action of 21 h in this model.
Animal Model: Sprague–Dawley rats[1]
Dosage: 10 mg/kg
Administration: 10 mg/kg; p.o.; twice daily; 7 days
Result: Significantly shortened path length when administered chronically compared to vehicle and administered acutely.
Molecular Weight

523.21

Formula

C17H18Br2FN3O3S
CAS No.
SMILES

O=S(C1=CC=C(C(N2CCNCC2)=C1)OC)(NC3=CC(Br)=CC(F)=C3Br)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (191.13 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9113 mL 9.5564 mL 19.1128 mL
5 mM 0.3823 mL 1.9113 mL 3.8226 mL
View the Complete Stock Solution Preparation Table

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  • Dilution Calculator

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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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (9.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (9.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9113 mL 9.5564 mL 19.1128 mL 47.7820 mL
5 mM 0.3823 mL 1.9113 mL 3.8226 mL 9.5564 mL
10 mM 0.1911 mL 0.9556 mL 1.9113 mL 4.7782 mL
15 mM 0.1274 mL 0.6371 mL 1.2742 mL 3.1855 mL
20 mM 0.0956 mL 0.4778 mL 0.9556 mL 2.3891 mL
25 mM 0.0765 mL 0.3823 mL 0.7645 mL 1.9113 mL
30 mM 0.0637 mL 0.3185 mL 0.6371 mL 1.5927 mL
40 mM 0.0478 mL 0.2389 mL 0.4778 mL 1.1945 mL
50 mM 0.0382 mL 0.1911 mL 0.3823 mL 0.9556 mL
60 mM 0.0319 mL 0.1593 mL 0.3185 mL 0.7964 mL
80 mM 0.0239 mL 0.1195 mL 0.2389 mL 0.5973 mL
100 mM 0.0191 mL 0.0956 mL 0.1911 mL 0.4778 mL
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SB357134 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SB357134219963-52-7SB 357134SB-3571345-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorRatbrain penetrant5-HT6 receptorInhibitorinhibitorinhibit

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