NTRC-824 

NTRC-824 (Compound 5) is a potent, selective and neurotensin-like nonpeptide neurotensin receptor type 2 (NTS2) antagonist with an IC₅₀ of 38 nM and a K_i of 202 nM. NTRC-824 is >150-fold selectivity for NTS2 over NTS1 (K_i >30 μM)^[1].

IC50: 38 nM (Nurotensin receptor type 2)^[1]
Ki: 202 nM (Nurotensin receptor type 2)^[1]

Testing of NTRC-824 (Compound 5) at the NTS1 receptor shows no binding activity in the NTS1 assay up to 30 μM, making NTRC-824 (Compound 5) selective for NTS2 in both the binding and functional assays. NTRC-824 (Compound 5) is the first nonpeptide compound that behaves like, and is more active than, the endogenous ligand^[1].

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

553.55

C₂₅H₂₆F₃N₃O₆S

1623002-61-8

Solid

Off-white to light yellow

CC(C)C[C@@H](C(O)=O)NC(CN1C=C(C(C(F)(F)F)=O)C2=C1C=CC(NS(=O)(C3=CC=C(C)C=C3)=O)=C2)=O

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Thomas JB, et al. Identification of N-[(5-{[(4-methylphenyl)sulfonyl]amino}-3-(trifluoroacetyl)-1H-indol-1-yl)acetyl]-l-leucine (NTRC-824), a neurotensin-like nonpeptide compound selective for the neurotensin receptor type 2. J Med Chem. 2014 Sep 11;57(17  [Content Brief]