Tropisetron

Catalog No.S5538 Batch:S553801

Technical Data

Formula	C₁₇H₂₀N₂O₂
Molecular Weight	284.35	CAS No.	89565-68-4
Solubility (25°C)*	In vitro	Water	56 mg/mL (196.94 mM)
		DMSO	10 mg/mL (35.16 mM)

* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.

Targets

5-HT3 receptor ^[1]	α7 nAChR ^[1]
5.3 nM(Ki)	6.9 nM(Ki)

In vitro

Tropisetron inhibits antigen-induced proliferation and IL-2 production in human peripheral T cells. Tropisetron inhibits the signalling pathways that regulate the activation of the transcription factors NFAT, NF-κB and AP-1, which are known to play a critical role in the immune response^[2].

In vivo

Tropisetron could ameliorate the ischemic brain injury via decreasing myeloperoxidase activity and TNF-α level. Tropisetron elicits anti-inflammatory effects in experimental model of cisplatin-induced nephrotoxicity and these effects were completely 5-HT3-receptor-independent^[3].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines Jurkat cells Concentrations 10, 25, 50 μg/ml Incubation Time 30 min Method Jurkat cells (1 × 10⁶ cells/ml) were stimulated with either TNFα (2 ng/ml) or PMA (20 ng/ml) plus ionomycin (0.5 ug/ml) for p65, JNK, ERK1 + 2, p38 and IκBα proteins in the presence or absence of tropisetron. Cells were then washed with PBS and proteins extracted in 50 μl of lysis buffer containing 0.5% NP-40. Protein concentration was determined by the Bradford assay and 30 μg of proteins were boiled in Laemmli buffer and electrophoresed in 10% SDS/polyacrylamide gels.
Animal Study:^{^[3]}	Animal Models Male albino mice Dosages 3 mg/kg Administration i.p.

Cell Assay:^{^[2]}

Cell lines
Jurkat cells
Concentrations
10, 25, 50 μg/ml
Incubation Time
30 min
Method
Jurkat cells (1 × 10⁶ cells/ml) were stimulated with either TNFα (2 ng/ml) or PMA (20 ng/ml) plus ionomycin (0.5 ug/ml) for p65, JNK, ERK1 + 2, p38 and IκBα proteins in the presence or absence of tropisetron. Cells were then washed with PBS and proteins extracted in 50 μl of lysis buffer containing 0.5% NP-40. Protein concentration was determined by the Bradford assay and 30 μg of proteins were boiled in Laemmli buffer and electrophoresed in 10% SDS/polyacrylamide gels.

Animal Study:^{^[3]}

Animal Models
Male albino mice
Dosages
3 mg/kg
Administration
i.p.

References

Selleck's Tropisetron has been cited by 1 publication

Inhibiting 5-hydroxytryptamine receptor 3 alleviates pathological changes of a mouse model of Alzheimer's disease [ Neural Regen Res, 2023, 18(9):2019-2028]	PubMed: 36926728

Inhibiting 5-hydroxytryptamine receptor 3 alleviates pathological changes of a mouse model of Alzheimer's disease [ Neural Regen Res, 2023, 18(9):2019-2028]

PubMed: 36926728

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SHIPPING AND STORAGE
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