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MedChemExpressModel Tropisetron Hydrochloride - 105826-92-4

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Tropisetron Hydrochloride (SDZ-ICS-930) is an effective neuroprotective agent that acts as a 5-HT3 receptor antagonist, a calmodulin inhibitor, and an α7-nAChRreceptor agonist, with an IC50 of 70.1 nM for the 5-HT3 receptor. Tropisetron Hydrochloride has anti-inflammatory properties and immune-regulating functions, effectively alleviating symptoms associated with chemotherapy and post-surgery. Tropisetron Hydrochloride reduces Ab (HY-P4867)-induced hippocampal neuroinflammation[1][2][3][4].
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Tropisetron Hydrochloride

MCE China:Tropisetron Hydrochloride

Brand:MedChemExpress (MCE)

Cat. No.HY-B0020

CAS:105826-92-4

Synonyms:SDZ-ICS-930

Purity:99.97%

Storage:4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

Description:Tropisetron Hydrochloride (SDZ-ICS-930) is an effective neuroprotective agent that acts as a 5-HT3 receptor antagonist, a calmodulin inhibitor, and an α7-nAChRreceptor agonist, with an IC50 of 70.1 nM for the 5-HT3 receptor. Tropisetron Hydrochloride has anti-inflammatory properties and immune-regulating functions, effectively alleviating symptoms associated with chemotherapy and post-surgery. Tropisetron Hydrochloride reduces Ab (HY-P4867)-induced hippocampal neuroinflammation.

In Vitro:Tropisetron Hydrochloride (1-1000 nM, 1 h) has a neuroprotective effect against glutamate-induced excitotoxicity in pig retinal ganglion cells (RGCs), with an EC50 of 62 nM[1]. Tropisetron Hydrochloride (100 nM, 1 h) does not have a significant impact on the pAkt levels in RGCs, but it significantly lowers the p38 MAPK levels associated with excitotoxicity[1]. Tropisetron Hydrochloride (1 nM-10 mM, 4 days) inhibits phosphatase activity in cerebellar granule neurons (CGNs)[2]. Tropisetron Hydrochloride (1 nM-10 mM, 4 days) does not affect the viability of CGNs[2]. Tropisetron Hydrochloride (10 nM-10 μM, 4 days) inhibits phosphatase activity in CGNs, increases CB1 expression, and reduces cAMP levels[2].

In Vivo:Tropisetron Hydrochloride (5 mg/kg, intraperitoneal injection, once daily for 32 days) has immunomodulatory effects in mice with experimental autoimmune encephalomyelitis (EAE)[3]. Tropisetron Hydrochloride (1 μg, ICV, single dose) reverses cognitive deficits in rats, providing protection against Ab (HY-P4867) induced neurotoxicity through both 5-HT3 receptor-dependent and independent pathways[4].

IC50 & Target:5-HT3 Receptor 70.1 nM (IC50) 5-HT3 Receptor α7-nAChR

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References:

[1]. Swartz MM, et al. Tropisetron as a neuroprotective agent against glutamate-induced excitotoxicity and mechanisms of action. Neuropharmacology. 2013 Oct;73:111-21.  [Content Brief]

[2]. Rahimian R, et al. Tropisetron upregulates cannabinoid CB1 receptors in cerebellar granule cells: possible involvement of calcineurin. Brain Res. 2011 Oct 12;1417:1-8.  [Content Brief]

[3]. Aminian A, et al. Tropisetron diminishes demyelination and disease severity in an animal model of multiple sclerosis. Neuroscience. 2013 Jun 15;248C:299-306.  [Content Brief]

[4]. Rahimian R, et al. Tropisetron attenuates amyloid-beta-induced inflammatory and apoptotic responses in rats. Eur J Clin Invest. 2013 Oct;43(10):1039-51.  [Content Brief]

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