1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Tropisetron Hydrochloride

Tropisetron Hydrochloride (Synonyms: SDZ-ICS-930)

Cat. No.: HY-B0020 Purity: 99.95%
Handling Instructions

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

For research use only. We do not sell to patients.

Tropisetron Hydrochloride Chemical Structure

Tropisetron Hydrochloride Chemical Structure

CAS No. : 105826-92-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 96 In-stock
Estimated Time of Arrival: December 31
100 mg USD 120 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Tropisetron Hydrochloride (SDZ-ICS-930) is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. IC50 value: 70.1 ± 0.9 nM Target: 5-HT3 receptor; α7-nicotinic receptor in vitro: Retinal ganglion cells(RGCs) pretreated with 100 nM tropisetron before glutamate increased cell survival to an average of 105% compared to controls. Inhibition studies using the alpha7 nAChR antagonist, MLA (10 nM), support the hypothesis that tropisetron is an effective neuroprotective agent against glutamate-induced excitotoxicity; mediated by α7 nAChR activation. Tropisetron had no discernible effects on pAkt levels but significantly decreased p38 MAPK levels associated with excitotoxicity from an average of 15 ng/ml to 6 ng/ml [2]. Tropisetron, but not granisetron, significantly inhibits the phosphatase activity of calcineurin, over-expresses the CB(1) receptors at both transcriptional and protein levels, and reduces cAMP content in cerebellar granule neurons (CGNs) [4]. in vivo: Animals were treated intracerebroventricularly with tropisetron, mCPBG (selective 5-HT3 receptor agonist) or mCPBG plus tropisetron on days 1, 3, 5 and 7. Tropisetron significantly diminished the elevated levels of these markers and reversed the cognitive deficit. Interestingly, tropisetron was also found to be a potent inhibitor of calcineurin phosphatase activity [1]. tropisetron (5mg/kg/day) plus mCPBG (10mg/kg/day), and granisetron (5mg/kg/day) intraperitoneally on days 3-35 post-immunization. Treatment with tropisetron and granisetron markedly suppressed the clinical symptoms of EAE (p<0.001) and reduced leukocyte infiltration as well as demyelination in the spinal cord (p<0.05) [3].

IC50 & Target

5-HT3 Receptor

70.1 nM (IC50)

Clinical Trial
Molecular Weight

320.81

Formula

C₁₇H₂₁ClN₂O₂

CAS No.

105826-92-4

SMILES

O=C(C1=CNC2=C1C=CC=C2)O[[email protected]]3C[[email protected]]4CC[[email protected]](N4C)C3.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

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

H2O : ≥ 50 mg/mL (155.86 mM)

DMSO : 33.33 mg/mL (103.89 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1171 mL 15.5855 mL 31.1711 mL
5 mM 0.6234 mL 3.1171 mL 6.2342 mL
10 mM 0.3117 mL 1.5586 mL 3.1171 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  PBS

    Solubility: 120 mg/mL (374.05 mM); Clear solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
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Keywords:

TropisetronSDZ-ICS-9305-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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Product Name:
Tropisetron Hydrochloride
Cat. No.:
HY-B0020
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