Tegaserod

SKU: orb2900865

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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 145158-71-0
• MW: 301.39
• Purity: >98% (HPLC)
• Formula: C₁₆H₂₃N₅O
• SMILES: N=C(NN=CC1=CNC=2C=CC(OC)=CC12)NCCCCC
• Target: 5-HT Receptor
• Solubility: In Vitro: DMSO : 50 mg/mL (165.90 mM; Ultrasonic )

Bioactivity

• In Vivo:
  Animal model: C57BL/6 J mice were subcutaneously injected with B16F10 cells. 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. 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).
• In Vitro:
  Apoptosis Analysis 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. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

5-HT Receptor