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

Tegaserod maleate  (Synonyms: SDZ-HTF-919; HTF-919)

Cat. No.: HY-14153A Purity: 99.93%
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Tegaserod maleate (SDZ-HTF-919) is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod maleate has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod maleate causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod maleate has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research.

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

Tegaserod maleate Chemical Structure

Tegaserod maleate Chemical Structure

CAS No. : 189188-57-6

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Based on 1 publication(s) in Google Scholar

Other Forms of Tegaserod maleate:

Tegaserod maleate 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 maleate (SDZ-HTF-919) is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod maleate has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod maleate causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod maleate has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research[1][2][3].

IC50 & Target

5-HT4 Receptor

 

5-HT2B Receptor

 

In Vitro

Tegaserod maleate (SDZ-HTF-919; 3-5 μM; 24-72 h) causes a significant time and dose-dependent increase in apoptosis[1].
Tegaserod maleate (3-5 μM; 8-18 h) decreases phosphorylation of the kinase directly upstream of S6, p70 S6 at Thr421/Ser424[1].
Tegaserod maleate (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 maleate 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 maleate (SDZ-HTF-919; 5 mg/kg/day; ip; for five consecutive days) delays tumor growth, reduces metastases, increases survival and suppresses p-S6 in vivo[1].
Tegaserod maleate (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

417.46

Formula

C20H27N5O5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(O)/C=C\C(O)=O.COC1=CC=C(NC=C2/C=N/NC(NCCCCC)=N)C2=C1
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 : ≥ 35 mg/mL (83.84 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3954 mL 11.9772 mL 23.9544 mL
5 mM 0.4791 mL 2.3954 mL 4.7909 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.

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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Volume (final)

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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: ≥ 2.5 mg/mL (5.99 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (5.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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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mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
%
Tween-80 +
%
Saline
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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 (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
DMSO 1 mM 2.3954 mL 11.9772 mL 23.9544 mL 59.8860 mL
5 mM 0.4791 mL 2.3954 mL 4.7909 mL 11.9772 mL
10 mM 0.2395 mL 1.1977 mL 2.3954 mL 5.9886 mL
15 mM 0.1597 mL 0.7985 mL 1.5970 mL 3.9924 mL
20 mM 0.1198 mL 0.5989 mL 1.1977 mL 2.9943 mL
25 mM 0.0958 mL 0.4791 mL 0.9582 mL 2.3954 mL
30 mM 0.0798 mL 0.3992 mL 0.7985 mL 1.9962 mL
40 mM 0.0599 mL 0.2994 mL 0.5989 mL 1.4971 mL
50 mM 0.0479 mL 0.2395 mL 0.4791 mL 1.1977 mL
60 mM 0.0399 mL 0.1996 mL 0.3992 mL 0.9981 mL
80 mM 0.0299 mL 0.1497 mL 0.2994 mL 0.7486 mL
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Tegaserod maleate 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:

Tegaserod189188-57-6SDZ-HTF-919 HTF-919HTF919HTF 919HTF-9195-HT ReceptorApoptosisSerotonin Receptor5-hydroxytryptamine Receptorserotonin receptorHTR45-HT45-HT2B5-HT2A5-HT2CPI3K/Akt/mTORS6irritable bowel syndromeIBSInhibitorinhibitorinhibit

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