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NTRC 824

Names

[ CAS No. ]:
1623002-61-8

[ Name ]:
NTRC 824

Biological Activity

[Description]:

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 Ki of 202 nM. NTRC-824 is >150-fold selectivity for NTS2 over NTS1 (Ki >30 μM)[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Neurotensin Receptor
Research Areas >> Neurological Disease

[Target]

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


[In Vitro]

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].

[References]

[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):7472-7.

Chemical & Physical Properties

[ Molecular Formula ]:
C25H26F3N3O6S

[ Molecular Weight ]:
553.55

Related Compounds