Tegaserod-d11

• Description:

  Tegaserod-d11 is deuterated labeled Tegaserod (HY-14153) . 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].

• UNSPSC:

  12352005

• Target:

  5-HT Receptor; Apoptosis; Isotope-Labeled Compounds

• Type:

  Isotope-Labeled Compounds

• Related Pathways:

  Apoptosis; GPCR/G Protein; Neuronal Signaling; Others

• Applications:

  Metabolism-protein/nucleotide metabolism

• Field of Research:

  Cancer; Metabolic Disease

• Solubility:

  10 mM in DMSO

• Smiles:

  N=C(NC([2H])([2H])C([2H])([2H])C([2H])([2H])C([2H])([2H])C([2H])([2H])[2H])N/N=C/C1=CNC2=CC=C(OC)C=C21

• Molecular Formula:

  C16H12D11N5O

• Molecular Weight:

  312.45

• References & Citations:

  [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.|[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.|[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.|[4]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Isotope-Labeled Compounds

• Clinical Information:

  No Development Reported

• Isoform:

  5-HT2 Receptor

• CAS Number:

  1134188-56-9