TAN-452

• Description :

  TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM) . TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control[1].

• UNSPSC :

  12352005

• Target :

  Opioid Receptor

• Type :

  Reference compound

• Related Pathways :

  GPCR/G Protein; Neuronal Signaling

• Applications :

  Neuroscience-Neuromodulation

• Field of Research :

  Neurological Disease

• Assay Protocol :

  https://www.medchemexpress.com/tan-452.html

• Purity :

  99.44

• Solubility :

  DMSO : 100 mg/mL (ultrasonic)

• Smiles :

  O=C(C1=CC2=C(C=C1)C3=C([C@@](OC4=C(O)C=CC(C5)=C46)([H])[C@]76[C@@]([C@]5([H])N(CC8CC8)CC7)(O)C3)N2)OCC

• Molecular Formula :

  C29H30N2O5

• Molecular Weight :

  486.56

• References & Citations :

  [1]Tsutomu Suzuki, et al. Pharmacological profile of TAN-452, a novel peripherally acting opioid receptor antagonist for the treatment of opioid-induced bowel syndromes. Life Sci. 2018 Dec 15;215:246-252.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  δ Opioid Receptor/DOR

• CAS Number :

  [892039-23-5]