TAN-452

• UNSPSC 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].

• Target Antigen:

  Opioid Receptor

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein;Neuronal Signaling

• Field of Research:

  Neurological Disease

• Assay Protocol:

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

• 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 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

• CAS Number:

  892039-23-5