1. Neuronal Signaling
  2. Dopamine Transporter Serotonin Transporter
  3. Tesofensine

Tesofensine  (Synonyms: NS-2330)

Cat. No.: HY-14472 Purity: 99.35%
COA Handling Instructions

Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM), and with potentials as an anti-obesity agent. Tesofensine is a CNS acting anti-obesity agent.

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

Tesofensine Chemical Structure

Tesofensine Chemical Structure

CAS No. : 195875-84-4

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Based on 1 publication(s) in Google Scholar

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Description

Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM), and with potentials as an anti-obesity agent[1]. Tesofensine is a CNS acting anti-obesity agent[2].

IC50 & Target

DA/NE/5-HT[1]

In Vivo

Tesofensine (a single dose of 0.1-3  mg/kg, s.c.) induces hypophagia in the DIO rat. A single dose of Tesofensine (0. 1-3 mg/kg, s.c.) robustly and dose dependently inhibits food intake in DIO rats over the 12 h nocturnal observation period. Daily administration of a moderate dose of Tesofensine (2.0 mg/kg, s.c.) over 16 days triggers a significant reduction in body weight after 4 days of administration relative to vehicle-treated controls[3].

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

Animal Model: Diet-induced obesity (DIO) rat[3]
Dosage: 0.1-3 mg/kg
Administration: Administered subcutaneously (s.c.); a single dose (acute treatment)
Result: The threshold dose for inhibition of total food intake was 1.0 mg/kg.
The ED50 for inhibition of total food intake in DIO rats was estimated to be 1.3 mg/kg.
Animal Model: Diet-induced obesity (DIO) rat[3]
Dosage: 2.0 mg/kg
Administration: Administered subcutaneously (s.c.) daily for over 16 days (chronic treatment)
Result: The average relative decrease in the body weight of tesofensine-treated DIO rats over the entire treatment period was 8.6±1.4%.
When comparing to vehicle controls, the relative weight loss with tesofensine was 13.8±1.4%.
Clinical Trial
Molecular Weight

328.28

Formula

C17H23Cl2NO

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN1[C@@]2([H])[C@H](COCC)[C@@H](C3=CC=C(Cl)C(Cl)=C3)C[C@]1([H])CC2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (6.09 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0462 mL 15.2309 mL 30.4618 mL
5 mM 0.6092 mL 3.0462 mL 6.0924 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

  • Protocol 1

    Tesofensine is dissolved in 0.9% saline solution[3].

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
Purity & Documentation
References

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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0462 mL 15.2309 mL 30.4618 mL 76.1545 mL
5 mM 0.6092 mL 3.0462 mL 6.0924 mL 15.2309 mL
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Tesofensine
Cat. No.:
HY-14472
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