Tegaserod maleate

SKU: orb1225822

Description

Tegaserod is a 5-HT4 agonist manufactured by Novartis and used for the management of irritable bowel syndrome and constipation. Its use was the only drug approved by the United States Food and Drug Administration to help relieve the abdominal discomfort, bloating and constipation associated with irritable bowel syndrome.

Key Properties

• CAS Number: 189188-57-6
• MW: 417.46
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₇N₅O₅
• SMILES: CCCCCN=C(N)NN/C=C/1\C=NC2=C1C=C(C=C2)OC.C(=C\C(=O)O)\C(=O)O
• Target: 5-HT Receptor
• Solubility: DMSO: 35mg/mL

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

Alternative Names

SDZ-HTF 919 | Zelnorm

Quick Database Links

Gene Symbol

5-HT Receptor