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

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

Cat. No.: HY-14153A Purity: 99.93%
COA Handling Instructions

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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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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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.

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)

H2O : 1 mg/mL (2.40 mM; Need ultrasonic)

*"≥" 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
10 mM 0.2395 mL 1.1977 mL 2.3954 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

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

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

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
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Tegaserod maleate Related Classifications

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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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Tegaserod maleate
Cat. No.:
HY-14153A
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