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145158-71-0-Tegaserod Tegaserod

Tegaserod

For research use only. Not for therapeutic Use.

  • CAT Number: M104362
  • CAS Number: 145158-71-0
  • Molecular Formula: C16H23N5O
  • Molecular Weight: 301.39
  • Purity: ≥95%
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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].
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].
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].


Catalog Number M104362
CAS Number 145158-71-0
Synonyms

1-[(E)-(5-methoxy-1H-indol-3-yl)methylideneamino]-2-pentylguanidine

Molecular Formula C16H23N5O
Purity ≥95%
InChI InChI=1S/C16H23N5O/c1-3-4-5-8-18-16(17)21-20-11-12-10-19-15-7-6-13(22-2)9-14(12)15/h6-7,9-11,19H,3-5,8H2,1-2H3,(H3,17,18,21)/b20-11+
InChIKey IKBKZGMPCYNSLU-RGVLZGJSSA-N
SMILES CCCCCN=C(N)NN=CC1=CNC2=C1C=C(C=C2)OC
Reference

[1]. Wei Liu, et al. Repurposing the serotonin agonist Tegaserod as an anticancer agent in melanoma: molecular mechanisms and clinical implications. J Exp Clin Cancer Res. 2020 Feb 21;39(1):38.
 [Content Brief]

[2]. M D Crowell, et al. The effects of tegaserod, a 5-HT receptor agonist, on gastric emptying in a murine model of diabetes mellitus. Neurogastroenterol Motil. 2005 Oct;17(5):738-43.
 [Content Brief]

[3]. D T Beattie, et al. The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Br J Pharmacol. 2004 Nov;143(5):549-60.
 [Content Brief]

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