Tropisetron-d5

Tropisetron-d5 (SDZ-ICS-930-d5 (free base) ) is deuterium labeled Tropisetron. Tropisetron (SDZ-ICS-930 free base) is an orally active anti-inflammatory and antiemetic agent. Tropisetron is 5-HT3R antagonists with a Ki of 5.3 nM. Tropisetron is also a partial agonist of α7 nicotinic receptor (α7 nAChR) with an EC50 of 1.3 μM. In addition, Tropisetron has antitumor and neuroprotective effects[1][2][3][4][5][6][7].

1220284-86-5

SDZ-ICS-930-d5 (free base)

12352005

5-HT Receptor; AP-1; Isotope-Labeled Compounds; JAK; nAChR; NF-κB; Nuclear Factor of activated T Cells (NFAT) ; p38 MAPK

Isotope-Labeled Compounds

Epigenetics; GPCR/G Protein; Immunology/Inflammation; JAK/STAT Signaling; MAPK/ERK Pathway; Membrane Transporter/Ion Channel; Neuronal Signaling; NF-κB; Others; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Cancer; Inflammation/Immunology; Neurological Disease

O=C(C1=C([2H])NC2=C1C([2H])=C([2H])C([2H])=C2[2H])O[C@H]3C[C@H]4CC[C@H](N4C)C3

C17H15D5N2O2

289.38

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.|[2]Macor JE, et al. The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist. Bioorg Med Chem Lett. 2001 Feb 12;11 (3) :319-21.|[3]Vega Lde L, et al. The 5-HT3 receptor antagonist tropisetron inhibits T cell activation by targeting the calcineurin pathway. Biochem Pharmacol. 2005 Aug 1;70 (3) :369-80.|[4]Stratz C, et al. The anti-inflammatory effects of the 5-HT? receptor antagonist tropisetron are mediated by the inhibition of p38 MAPK activation in primary human monocytes. Int Immunopharmacol. 2012 Aug;13 (4) :398-402.|[5]Guo L, et al. Tropisetron Ameliorated Cyclophosphamide-Induced Hemorrhagic Cystitis via Restraining TLR-4/NF-κB and JAK1/STAT3 Signaling Pathways. Arch Esp Urol. 2023 Feb;76 (1) :56-64.|[6]Rashidi M, et al. Tropisetron attenuates tumor growth and progression in an experimental model of mouse lung cancer. J Cell Biochem. 2020 Feb;121 (2) :1610-1622.|[7]Divanbeigi A, et al. Tropisetron But Not Granisetron Ameliorates Spatial Memory Impairment Induced by Chronic Cerebral Hypoperfusion. Neurochem Res. 2020 Nov;45 (11) :2631-2640.

Room temperature

Isotope-Labeled Compounds