Tesofensine

• UNSPSC 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].

• Target Antigen:

  Dopamine Transporter; Serotonin Transporter

• Type:

  Reference compound

• Related Pathways:

  Neuronal Signaling

• Applications:

  Metabolism-protein/nucleotide metabolism

• Field of Research:

  Metabolic Disease

• Assay Protocol:

  https://www.medchemexpress.com/tesofensine.html

• Solubility:

  DMSO : 2 mg/mL (ultrasonic;warming)

• Smiles:

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

• Molecular Weight:

  328.28

• References & Citations:

  [1]Lieuwe Appel, et al. Tesofensine, a novel triple monoamine re-uptake inhibitor with anti-obesity effects: dopamine transporter occupancy as measured by PET. Eur Neuropsychopharmacol. 2014 Feb;24(2):251-61.|[2]Ann A Coulter, et al. Centrally Acting Agents for Obesity: Past, Present, and Future. Drugs. 2018 Jul;78(11):1113-1132.|[3]Anne Marie D Axel, et al. Tesofensine, a novel triple monoamine reuptake inhibitor, induces appetite suppression by indirect stimulation of alpha1 adrenoceptor and dopamine D1 receptor pathways in the diet-induced obese rat.Neuropsychopharmacology. 2010 Jun;35(7):1464-76.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  Phase 2

• CAS Number:

  195875-84-4