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

Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research.

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Tegaserod Chemical Structure

Tegaserod Chemical Structure

CAS No. : 145158-71-0

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Based on 1 publication(s) in Google Scholar

Other Forms of Tegaserod:

Tegaserod Related Antibodies

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

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Description

Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research[1][2][3].

IC50 & Target

5-HT4 Receptor

 

In Vitro

Tegaserod (3-5 μM; 24-72 h) causes a significant time and dose-dependent increase in apoptosis[1].
Tegaserod (3-5 μM; 8-18 h) decreases phosphorylation of the kinase directly upstream of S6, p70 S6 at Thr421/Ser424[1].
Tegaserod (0.1-3 μM; 24h) inhibits 5-HT-mediated contraction of the rat isolated stomach fundus potently (pA2=8.3), consistent with 5-HT2B receptor antagonist activity[3].

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

Tegaserod Related Antibodies

Apoptosis Analysis[1]

Cell Line: A375, RPMI-7951 (RPMI), SH4, B16F10, MeWo and MEL-JUSO
Concentration: 3, 5 μM
Incubation Time: 24, 48, 72 h
Result: There was a significant time and dose-dependent increase in apoptosis in all cell lines.

Western Blot Analysis[1]

Cell Line: RPMI, SH4 and B16F10 cells
Concentration: 3, 5 μM
Incubation Time: 8 or 18 h
Result: Decreased phosphorylation of the kinase directly upstream of S6, p70 S6 at Thr421/Ser424.
In Vivo

Tegaserod (5 mg/kg/day; ip; for five consecutive days) delays tumor growth, reduces metastases, increases survival and suppresses p-S6 in vivo[1].
Tegaserod (0.1-2.0 mg/kg; IP 15 min prior to gastric loading) significantly accelerates the gastric emptying rate of glucose in db/db mice, reducing the fraction of the meal remaining in the stomach at 30 min by 80% with 0.1mg/kg[2].

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

Animal Model: C57BL/6 J mice were subcutaneously injected with B16F10 cells[1]
Dosage: 5 mg/kg
Administration: Administered intraperitoneally (i.p.) daily for five consecutive days
Result: Treatment significantly decreased tumor growth and resulted in only slight decreases in weight following treatment.
Animal Model: Female C57BLKS/J db/db mice[2]
Dosage: 0.1, 0.5, 1.0, 2.0 mg/kg
Administration: IP 15 min prior to gastric loading
Result: Produced a dramatic decrease in the fraction of the meal remaining in the stomach for doses as low as 0.1 mg/kg (0.1 mg/kg).
Accelerated gastric emptying, with a reduction of nearly 80% in the fraction remaining at 30 min (P < 0.0001) (0.1 mg/kg).
Induced a significant decrease in the gastric emptying rate as the amount of the meal remaining at 30 min was significantly greater (2.0 mg/kg).
Resulted in inhibition of tegaserod-induced increased gastric emptying (0.1 mg/kg).
Clinical Trial
Molecular Weight

301.39

Formula

C16H23N5O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC1=CC=C(NC=C2/C=N/NC(NCCCCC)=N)C2=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (165.90 mM; Need ultrasonic; 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 3.3180 mL 16.5898 mL 33.1796 mL
5 mM 0.6636 mL 3.3180 mL 6.6359 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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:

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 (16.59 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (16.59 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 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.
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

* 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. 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 3.3180 mL 16.5898 mL 33.1796 mL 82.9490 mL
5 mM 0.6636 mL 3.3180 mL 6.6359 mL 16.5898 mL
10 mM 0.3318 mL 1.6590 mL 3.3180 mL 8.2949 mL
15 mM 0.2212 mL 1.1060 mL 2.2120 mL 5.5299 mL
20 mM 0.1659 mL 0.8295 mL 1.6590 mL 4.1474 mL
25 mM 0.1327 mL 0.6636 mL 1.3272 mL 3.3180 mL
30 mM 0.1106 mL 0.5530 mL 1.1060 mL 2.7650 mL
40 mM 0.0829 mL 0.4147 mL 0.8295 mL 2.0737 mL
50 mM 0.0664 mL 0.3318 mL 0.6636 mL 1.6590 mL
60 mM 0.0553 mL 0.2765 mL 0.5530 mL 1.3825 mL
80 mM 0.0415 mL 0.2074 mL 0.4147 mL 1.0369 mL
100 mM 0.0332 mL 0.1659 mL 0.3318 mL 0.8295 mL
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Tegaserod 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:

Tegaserod145158-71-05-HT ReceptorApoptosisSerotonin Receptor5-hydroxytryptamine Receptorserotonin receptorHTR45-HT45-HT2B5-HT2A5-HT2CPI3K/Akt/mTORS6irritable bowel syndromeIBSInhibitorinhibitorinhibit

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