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> Tropisetron (Hydrochloride) [105826-92-4]

Tropisetron (Hydrochloride) [105826-92-4]

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Cat# HY-B0020-100mg

Size : 100mg

Brand : MedChemExpress

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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[1][2][3][4].

IC50 & Target

5-HT3 Receptor

70.1 nM (IC50)

5-HT3 Receptor

 

α7-nAChR

 

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tropisetron Hydrochloride Related Antibodies

Cell Viability Assay[1][2]

Cell Line: Pig RGCs induced by glutamate[1]; CGNs[2]
Concentration: 1, 10, 50, 100, 1000 nM; 1, 10, 100, 1000, 10000, 100000, 1000000 nM
Incubation Time: 1 h; 4 days
Result: Increased RGCs cell survival rate.
Had no effect on CGNs cell vitality at 1nM-10mM; higher doses reduced cell vitality.

Western Blot Analysis[2]

Cell Line: CGNs (rat)
Concentration: 100 nM, 1 μM, 10 μM
Incubation Time: 4 days
Result: Inhibited the activity of calcineurin, increased the expression of CB1, and reduced cAMP levels.

Real Time qPCR[2]

Cell Line: CGNs (rat)
Concentration: 100 nM, 1 μM, 10 μM
Incubation Time: 4 days
Result: Inhibited the activity of calcineurin, increased the expression of CB1, and reduced cAMP levels.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Beta-amyloid (Ab) rat model of AD[4]
Dosage: 1 μg, single dose
Administration: Intracerebroventricular injection (ICV)
Result: Increased in TNF-a, COX-2, iNOS, NF-κB, active caspase 3, cytochrome c release and calcineurin phosphatase activity in the hippocampus.
Animal Model: Rxperimental autoimmune encephalomyelitis (EAE) mice induced by myelin oligodendrocyte glycoprotein peptide[3]
Dosage: 5 mg/kg, daily, 32 days
Administration: Intraperitoneal injection (i.p.)
Result: Improved the clinical symptoms of EAE, suppressed the infiltration of inflammatory cells in the central nervous system and demyelination, significantly reduced the number and extent of inflammatory lesions and demyelinated areas, decreased the quantity and function of effector T cells, and inhibited the production of pro-inflammatory cytokines IL-17, IL-6, and IL-2.
Clinical Trial
Molecular Weight

320.81

Formula

C17H21ClN2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CNC2=C1C=CC=C2)O[C@H]3C[C@H]4CC[C@H](N4C)C3.13Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 70 mg/mL (218.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 50 mg/mL (155.86 mM)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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