1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. TCB2

TCB2 is an agonist of serotonin 5-HT2A receptor.

For research use only. We do not sell to patients.

TCB2 Chemical Structure

TCB2 Chemical Structure

CAS No. : 912342-28-0

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5 mg USD 150 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

TCB2 is an agonist of serotonin 5-HT2A receptor.

IC50 & Target

5-HT2A Receptor

 

In Vitro

The selective 5-HT2A agonist TCB2 at 30 nM produces a marked shift to the right in the competition curve obtained with the 5-HT1A receptor agonist ipsapirone from [3H]-8-OHDPAT binding sites in both areas of the brain. A significant increase in the mean Ki value is obtained with TCB2, demonstrating a reduction in the affinity of the high-affinity 5-HT1A agonist binding sites by the 5-HT2A agonist in both regions. In the case of hippocampus, there are also indications for antagonistic effects of ketanserin[2].

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

In Vivo

In an initial dose-response study, TCB2 (0.5, 1.0, and 2.5 mg/kg) and DOI (0.5, 1.0, 2.5, and 5.0 mg/kg) induce head twitches in C57BL/6J mice in a dose-dependent manner compared to vehicle. Head twitches induced by TCB2 and DOI are similar across the doses, with the exception that at the highest dose (5.0 mg/kg), TCB2 induces half as many head twitches as does DOI (p=0.021). Confirming 5-HT2A mediation of the head twitch response, in two separate studies, pretreatment with the selective 5-HT2A antagonist MDL 11,939 (1.0 mg/kg) block head twitches induced by DOI (2.5 mg/kg) and by TCB2 (2.5 mg/kg; p<0.0001). Compared to vehicle, corticosterone levels are increased following TCB2 (5.0 mg/kg, p=0.01; 10.0, p=0.012; with a trend following 2.5 mg/kg, p=0.079) and DOI (10.0 mg/kg, p=0.035)[1].

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

Molecular Weight

353.05

Formula

C11H15Br2NO2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NCC1C2=C(OC)C=C(Br)C(OC)=C2C1.[H]Br

Shipping

Room temperature in continental US; may vary elsewhere.

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
In Vitro: 

DMSO : 100 mg/mL (283.25 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)

H2O : 25 mg/mL (70.81 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8325 mL 14.1623 mL 28.3246 mL
5 mM 0.5665 mL 2.8325 mL 5.6649 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.21%

References
Animal Administration
[1]

Mice[1]
Male C57BL/6J mice and SERT+/+ (+/−, −/−) mice (25-30 g) are used. TCB2 is dissolved in distilled water, MDL 11,939 is dissolved in a few drops of acetic acid and prepared in distilled water, and DOI is dissolved in saline. All drugs and their vehicles are administered via intraperitoneal injection at a volume of 10 ml/kg. Following 15 min of habituation in a plexiglass container, mice are administered the test drug. Head twitches were recorded for five 1-min periods over a 30-min period; the scores from the five 1-min periods are summed together. In two separate experiments, mice are pretreated with the selective 5-HT2A antagonist MDL 11,939 (1.0 mg/kg) or its vehicle 30 min prior to administration of DOI or TCB2 (2.5 mg/kg). Finally, head twitches are assessed in SERT+/+ (+/−, −/−) mice administered TCB2. C57BL/6J mice are injected with vehicle, TCB2 (1.0 or 2.5 mg/kg) or DOI (1.0 or 2.5 mg/kg). Following administration of vehicle, TCB2 (1.0, 2.5, or 5.0 mg/kg) or DOI (1.0, 2.5, or 5.0 mg/kg), mice are placed in the test cage. In a final feeding study, mice are pretreated with vehicle or MDL 11,939 (1.0 mg/kg) followed 30 min later by an intermediate dose of TCB2 (3.75 mg/kg)[1].

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

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 2.8325 mL 14.1623 mL 28.3246 mL 70.8115 mL
5 mM 0.5665 mL 2.8325 mL 5.6649 mL 14.1623 mL
10 mM 0.2832 mL 1.4162 mL 2.8325 mL 7.0812 mL
15 mM 0.1888 mL 0.9442 mL 1.8883 mL 4.7208 mL
20 mM 0.1416 mL 0.7081 mL 1.4162 mL 3.5406 mL
25 mM 0.1133 mL 0.5665 mL 1.1330 mL 2.8325 mL
30 mM 0.0944 mL 0.4721 mL 0.9442 mL 2.3604 mL
40 mM 0.0708 mL 0.3541 mL 0.7081 mL 1.7703 mL
50 mM 0.0566 mL 0.2832 mL 0.5665 mL 1.4162 mL
60 mM 0.0472 mL 0.2360 mL 0.4721 mL 1.1802 mL
DMSO 80 mM 0.0354 mL 0.1770 mL 0.3541 mL 0.8851 mL
100 mM 0.0283 mL 0.1416 mL 0.2832 mL 0.7081 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.

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  • 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.

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TCB2
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