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MedChemExpress - Model Tropisetron - ...

MedChemExpress - Model Tropisetron - 89565-68-4

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].

Tropisetron

MCE China：Tropisetron

Brand：MedChemExpress (MCE)

Cat. No.HY-B0072

CAS：89565-68-4

Synonyms：SDZ-ICS-930 free base

Purity：98.72%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：ropisetron (10-50 μg/mL; 72 h) inhibits T cell activation in human peripheral T cells[2]. Tropisetron (10-50 μg/mL; 30 min) inhibits the activation of NFAT, AP-1, NF-κB and IL-2 production in Jurkat cells[2]. Tropisetron (1-50 μg/mL; 4 h) decreases the phosphorylation level of p38 MAPK in human monocytes treated with LPS (HY-D1056)[3].

In Vivo：Tropisetron (2.5-7.5mg /kg; Intraperitoneal injection; 5 days) has an improved effect in a rat model of hemorrhagic cystitis induced by cyclophosphamide (HY-17420)[4]. Tropisetron (5-10 mg/kg; Intraperitoneal injection; 10-22 days) has antitumor effect in lung cancer mouse model[5]. Tropisetron (1-5 mg/kg; Intraperitoneal injection; 35 days) improves the spatial memory impairment induced by chronic cerebral hypoperfusion in rat models[6].

IC50 & Target：5-HT3 Receptor 5.3 nM (Ki)

References：

[1]. 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. [Content Brief]

[2]. 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. [Content Brief]

[3]. 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. [Content Brief]

[4]. 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. [Content Brief]

[5]. 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. [Content Brief]

[6]. 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. [Content Brief]

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