Tesofensine CAS No. 195875-84-4

Product Description

Warning: This product is for research use only and is not for clinical use.

Tesofensine is a Phase II small-molecule triple monoamine re-uptake inhibitor that was first explored for Alzheimer’s and Parkinson’s diseases but has been repositioned as a promising anti-obesity agent. By simultaneously blocking the reuptake of serotonin, noradrenaline and dopamine, it potently curbs appetite, enhances satiety and may boost metabolic rate. In clinical trials, participants lost up to 10–12 % of body weight (~9–11 kg) over six months—outperforming orlistat and rivaling GLP-1 agonists such as semaglutide, yet via a centrally acting CNS mechanism rather than peripheral pathways. Common adverse effects include dry mouth, nausea, insomnia and mild cardiovascular elevations, while long-term safety is still under investigation. Originally developed by NeuroSearch (Denmark), development rights now reside with Saniona, which is advancing tesofensine through additional trials toward potential regulatory approval.

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Product Use & Characteristics

Basic Chemistry & Identification

Item	Data
Chemical Name	(1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane
Molecular Formula	C₁₇H₂₃Cl₂NO
Molecular Weight	328.3 g/mol
Synonyms / Codes	NS 2330; Tesofensine (INN)

Mechanism of Action

• Triple monoamine re-uptake inhibitor

  • DAT (Dopamine transporter) IC₅₀ ≈ 6.5 nM

  • NET (Norepinephrine transporter) IC₅₀ ≈ 1.7 nM

  • SERT (Serotonin transporter) IC₅₀ ≈ 11 nM

• Active metabolite M1 (NS 2360) shows even higher potency: NET 0.6 nM, SERT 2.0 nM, DAT 3.0 nM.

• Functional consequences

  • ↑ extracellular DA, NE, 5-HT → ↑ satiety, ↓ appetite, ↑ energy expenditure.

  • PET imaging shows dose-dependent striatal DAT occupancy 18–77 % (0.25–1 mg/day).

Pharmacology & Pre-clinical Highlights

Model	Key Findings
Diet-Induced Obese (DIO) rats	• 5.7–9.9 % sustained weight-loss (1–2.5 mg/kg p.o., 28 days)
Lean vs Obese rats	• Greater weight-loss efficacy in obese animals
Behavioural & neurophysiology	• Silences lateral hypothalamic GABAergic neurons that drive feeding

Clinical Experience

Trial / Phase	Outcome
Phase II obesity (0.25–1 mg/day, 24 wks)	• 10.6 % placebo-adjusted weight-loss (1 mg)
Phase II Parkinson’s / Alzheimer’s	• Insufficient efficacy for primary endpoints; marked, unintended weight-loss observed → pivot to obesity indication
PET study (healthy males)	• ED₅₀ for striatal DAT occupancy ≈ 0.25 mg TE; Cp ≈ 4 ng/mL

Uses (Approved / Investigational)

• Primary Development: Anti-obesity therapy (Phase II completed).

• Secondary / Repurposed:

  • Hypothalamic obesity (rare disorder, ongoing Phase IIb).

  • Adjunct to serotonin precursors (e.g., 5-HTP/CB) – prevents weight-rebound.

Safety & Tolerability

Dose	Observations
Therapeutic (≤ 2 mg/day)	• Mild cardiovascular stimulation (↑ HR/BP)
Supra-therapeutic (6 mg/kg in rats)	• Stereotypic tongue movements / locomotor reduction

Why us!

Qingdao Sigma Chemical Co., Ltd., established in January 2017 and headquartered in Qingdao, China, is a reliable chemical supplier. Specializing in pharmaceuticals, biochemical intermediates, and research chemicals, the company offers a diverse product portfolio, including peptides (e.g., Tirzepatide, Semaglutide), nootropics, veterinary products, and APIs, often marketed with ≥99% purity and COA certification. We provides R&D, custom synthesis, and contract manufacturing services at various scales, while claiming a global export presence across 100+ countries. With international warehouses in the USA, Europe, Australia, and Canada, Qingdao Sigma Chemical also facilitates drop-shipping and reshipments, positioning itself as a key supplier for laboratory and research applications.