1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor
  3. TAN-452

TAN-452 

Cat. No.: HY-136208
Handling Instructions

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.

For research use only. We do not sell to patients.

TAN-452 Chemical Structure

TAN-452 Chemical Structure

CAS No. : 892039-23-5

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

IC50 & Target

Ki: 0.47 nM (DOR), 36.56 nM (MOR) and 5.31 nM (KOR)[1]
Kb: 0.21 nM (DOR), 9.43 nM (MOR) and 7.18 nM (KOR)[1]

In Vivo

TAN-452 (1, 3, 10 mg/kg for p.o. or 0.3, 1, 3 mg/kg for s.c.) suppresses morphine-induced emesis in ferrets[1].
TAN-452 (30 mg/kg/2 mL for PO or 3 mg/kg/mL for IV) has a T1/2 of 2.1 hours[1].
TAN-452 suppresses morphine-induced small intestinal transit (SIT) inhibition in a dose-dependent manner. Administration of TAN-452 at 30 mg/kg alone does not affect SIT[1].
TAN-452 (10, 30 mg/kg; s.c.) significantly suppresses morphine-induced antinociception 30 min after administration. TAN-452 (po) produces no effect up to 300 mg/kg[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male ferrets (1.3-1.9 kg)[1]
Dosage: 1, 3, 10 mg/kg (p.o.) or 0.3, 1, 3 mg/kg (s.c.)
Administration: PO or SC; before morphine
Result: Prevented morphine-induced emesis in half of the animals with orally administered of 1 mg/kg and completely abolished emesis at 3 and 10 mg/kg.
Completely abolished emesis by subcutaneous injection at 0.3, 1, and 3 mg/kg.
Animal Model: Crj:CD(SD) IGS male rats (7 weeks old)[1]
Dosage: 30 mg/kg/2 mL for PO or 3 mg/kg/mL for IV (Pharmacokinetic Analysis)
Administration: Orally or intravenously
Result: Had a T1/2 of 2.1 hours, a CL of 78.1 mL/min•kg, a Vss of 12.1 L/kg, and a Cmax of 526 ng/mL.
Molecular Weight

486.56

Formula

C₂₉H₃₀N₂O₅

CAS No.

892039-23-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

TAN-452TAN452TAN 452Opioid Receptororallyδ-opioidreceptorDORμ-opioidMORκ-opioidKORNaltrindolemorphineantinociceptionInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
TAN-452
Cat. No.:
HY-136208
Quantity:
MCE Japan Authorized Agent: