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TAN-452

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].

Product Specifications

CAS Number

[892039-23-5]

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

Available Sizes

Curated Selection

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