Novera Tesofensine 30 tablets 500mcg

Tesofensine (NS-2330) is a potent triple monoamine reuptake inhibitor that blocks the presynaptic transporters for dopamine (DAT), norepinephrine (NET), and serotonin (SERT), elevating synaptic concentrations of all three neurotransmitters simultaneously. Originally developed by NeuroSearch A/S for neurodegenerative disease research, this research compound rapidly gained attention when early clinical evaluations revealed pronounced effects on appetite suppression and body weight reduction, redirecting scientific interest toward obesity, metabolic pathway research, and reward circuit investigations. Tesofensine is an experimental triple monoamine reuptake inhibitor currently in Phase 3 clinical trials for obesity, and it is studied extensively for monoamine transporter activity, appetite-related signaling research, and CNS pathway modulation in controlled laboratory settings.

This molecule is supplied by FillerSupplies.com under the Novera brand intended strictly for laboratory research and qualified professionals conducting preclinical or in-vitro investigations. Tesofensine is for laboratory research use only and is not intended for human or veterinary consumption. It is not FDA-approved for obesity treatment in the United States, and the U.S. FDA has warned against marketing tesofensine as a dietary supplement. Buying tesofensine online poses significant health and legal risks due to its lack of FDA approval when sourced from unverified sellers, which is why researchers seeking to buy tesofensine should rely exclusively on established, quality-controlled suppliers with verifiable batch documentation and consistency in their manufacturing process.

General Information About Tesofensine

Tesofensine belongs to the phenyltropane family of small molecules – it is not a peptide but a synthetic compound with the molecular formula C₁₇H₂₃Cl₂NO and a molecular weight of 328.28 g/mol. Its citrate salt form (tesofensine citrate), commonly used in research preparations, has the molecular formula C₂₃H₃₁Cl₂NO₈ and a molecular weight of approximately 520.4 g/mol. The compound was originally developed by NeuroSearch A/S (Denmark) as a potential therapeutic candidate for Parkinson’s disease and Alzheimer’s disease. During Phase II clinical evaluation for neurodegenerative conditions, investigators observed significant and unexpected weight loss among trial participants, prompting a strategic pivot toward metabolic and obesity-focused research applications.

The mechanism of action centers on triple reuptake inhibition: tesofensine blocks the presynaptic transporters responsible for clearing dopamine, norepinephrine, and serotonin from the synaptic cleft, thereby increasing extracellular concentrations of these monoamines across multiple CNS regions including the prefrontal cortex, hypothalamus, and nucleus accumbens. In vitro receptor binding profiles demonstrate IC₅₀ values of approximately 1.7 nM for NET, ~11 nM for SERT, and ~65 nM for DAT, indicating greatest potency at the norepinephrine transporter with moderate serotonergic and lower dopaminergic reuptake inhibition. Downstream, appetite suppression appears to be mediated primarily through indirect stimulation of α₁-adrenergic receptors and dopamine D₁ receptors – blockade studies in animal research models showed that co-administration of the α₁ antagonist prazosin almost completely reversed tesofensine-induced hypophagia.

In human pharmacokinetic studies, tesofensine demonstrates oral bioavailability exceeding 90% with linear kinetics across tested dose ranges. The parent compound has a half-life of approximately 8 days, while its primary metabolite (NS-2360, the desalkyl metabolite M1) exhibits a longer half-life of roughly 16 days, with steady-state exposure reaching about 31–34% of the parent compound. Hepatic metabolism occurs predominantly via CYP3A4, with renal clearance accounting for only 15–20% of elimination.

Compared to related compounds such as sibutramine (a dual norepinephrine/serotonin reuptake inhibitor with minimal DAT involvement) and lorcaserin (a selective 5-HT₂C receptor agonist rather than a classical reuptake inhibitor), tesofensine offers a more comprehensive triple reuptake profile. This broader monoamine modulation has been associated with stronger appetite suppression in controlled research settings while producing fewer stereotypic motor behaviors than traditional stimulants like phentermine, suggesting a potentially differentiated pharmacological profile for investigators studying food intake regulation and energy homeostasis.

Tesofensine Use in the Research Setting

Tesofensine is available in 500 mcg capsule format as well as lyophilized powder form for laboratory research use only, manufactured under cGMP standards for research applications. It is not intended for human consumption or medical use, and all experimental protocols should be conducted by qualified professionals operating under appropriate institutional oversight.

#1. Appetite Regulation and Metabolic Research

Animal studies using diet-induced obese (DIO) rat models have demonstrated that chronic tesofensine administration (1–2 mg/kg, subcutaneous, for 16–28 days) produces substantial reductions in food intake and body weight. At 2 mg/kg over 16 days, researchers observed approximately 14% body weight reduction with food intake suppression of roughly 49% versus vehicle controls. The ED₅₀ for hypophagia in nocturnal food intake was established at approximately 1.3 mg/kg subcutaneously. It is relevant for appetite-related signaling research and metabolic pathway research because mechanistic investigations have shown that tesofensine suppresses appetite via the hypothalamus, particularly by silencing a subset of GABAergic neurons in the lateral hypothalamus. A 2024 study by Perez, Luis-Islas, and colleagues confirmed that chemogenetic silencing of these same neuronal populations enhanced appetite suppression, further validating the hypothalamic target.

In Phase II human obesity trials, 203 obese participants receiving daily oral doses of 0.25, 0.5, or 1.0 mg for 24 weeks exhibited placebo-adjusted mean weight losses of approximately 6.7, 11.3, and 12.8 kg respectively, compared to 2.2 kg in the placebo group, along with improvements in lipid and glycemic parameters. When evaluated against other appetite research compounds, tesofensine’s triple reuptake mechanism distinguishes it from single- or dual-target agents, offering researchers a pharmacological tool to dissect the relative contributions of dopaminergic, noradrenergic, and serotonergic systems to feeding behavior.

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#2. Neurotransmitter Pathway Studies

Tesofensine serves as a valuable pharmacological probe for researchers investigating dopaminergic, noradrenergic, and serotonergic system interactions within the CNS. In DIO rat models, chronic administration reversed the characteristically low forebrain dopamine levels associated with diet-induced obesity, as measured by in vivo microdialysis. This normalization of extracellular dopamine was accompanied by alterations in dopamine receptor expression and transporter binding density, providing concrete evidence that obesity-associated monoamine deficits are pharmacologically reversible.

The compound’s differential selectivity profile – greatest potency at NET, moderate at SERT, and comparatively lower at DAT – allows researchers to parse the relative contributions of each monoamine system to specific behavioral and physiological outcomes. The strong noradrenergic component appears primarily responsible for appetite suppression and cardiovascular effects, the serotonergic modulation likely contributes to satiety signaling, and the dopaminergic action, while less potent in absolute reuptake terms, plays a critical role in reward circuit modulation. Blockade studies have confirmed that α₁-adrenoceptor antagonism largely reverses the hypophagic response, while DA D₁ receptor antagonism produces only partial reversal, with minimal involvement observed from α₂, D₂, D₃, or 5-HT₂A/C receptor blockade.

#3. Behavioral and Reward Circuit Research

Studies in DIO animal models have revealed that tesofensine reverses low basal dopamine levels in the nucleus accumbens and other mesolimbic reward areas. This finding indicates that tesofensine’s appetite-suppressing effects extend beyond classical satiety and energy homeostasis centers to include modulation of reward-driven feeding behavior – a critical distinction for researchers investigating the neurobiological overlap between obesity and addictive-like food consumption patterns.

Compared to stimulant-class compounds such as phentermine, tesofensine produced fewer stereotypic behaviors (e.g., head weaving, repetitive locomotion) in rodent models at research-relevant doses, suggesting a more favorable profile within reward and motor circuits. This observation is particularly significant for investigators designing chronic administration protocols, as it implies that tesofensine’s triple reuptake mechanism may achieve appetite modulation with less disruption to normal behavioral repertoires than single-target stimulants.

“Tesofensine treatment (1.5 mg/kg, s.c.) induced a robust hypophagic response in DIO rats, which was almost completely reversed by the α₁-adrenoceptor antagonist prazosin, and partially by a DA D₁ receptor antagonist.” – Axel et al., Neuropsychopharmacology, 2010

#4. Pharmacokinetic and Safety Profile Research

The pharmacokinetic profile of tesofensine is well-characterized in human research settings: greater than 90% oral bioavailability, linear kinetics across single and multiple doses, CYP3A4-mediated hepatic metabolism, and a uniquely long elimination half-life (~8 days for parent, ~16 days for the NS-2360 metabolite). These parameters are critical for researchers designing dosing intervals and washout periods in experimental protocols. Side effects of tesofensine observed in Phase II human trials may include dry mouth (up to ~47.7% of subjects), insomnia (1.9–24.6%), nausea (7.7–12.8%), diarrhea (7.7–12.6%), constipation (1.9–8.6%), increased heart rate (approximately 7–8 beats per minute above baseline in the 0.5–1.0 mg/day groups), and mild blood pressure changes. These safety parameters should inform risk assessments for any animal study protocol design.

Combination formulations have also entered the research pipeline: “Tesomet,” a combination of tesofensine with metoprolol (a β₁-adrenergic blocker), has been evaluated in Phase II trials for hypothalamic obesity, with the goal of mitigating cardiovascular side effects while preserving appetite-suppressive efficacy.

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Buy Tesofensine Online at FillerSupplies.com

When you need to buy tesofensine online for your laboratory research, FillerSupplies.com provides a trusted, established source with professional fulfillment and precision in every order. Whether you are investigating monoamine transporter activity, conducting appetite-related signaling experiments, or exploring metabolic pathway mechanisms, our Novera-brand tesofensine delivers the consistency and quality that serious researchers demand. Tesofensine 500MCG costs approximately $89.99 to $99.99, with pricing that varies based on purity, form, and testing protocols – and bulk orders may reduce the cost per unit of tesofensine through our tiered wholesale pricing structure.

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• Supplied for research use only, to licensed professionals.

Tesofensine is sold strictly for laboratory research use only. It is not intended for human or animal use, human consumption, diagnostic procedures, or therapeutic application. Legitimate suppliers of tesofensine should provide Certificates of Analysis for every lot, and independent third-party testing confirms tesofensine’s identity and purity – researchers should always verify batch documentation before incorporating any research compound into their experimental protocols. FDA-approved medications undergo regulatory review for safety, efficacy, and quality; tesofensine has not completed this process and remains an investigational compound.

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