For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I011197 |
| CAS Number | 1623002-61-8 |
| Synonyms | (2S)-4-methyl-2-[[2-[5-[(4-methylphenyl)sulfonylamino]-3-(2,2,2-trifluoroacetyl)indol-1-yl]acetyl]amino]pentanoic acid |
| Molecular Formula | C25H26F3N3O6S |
| Purity | ≥95% |
| InChI | InChI=1S/C25H26F3N3O6S/c1-14(2)10-20(24(34)35)29-22(32)13-31-12-19(23(33)25(26,27)28)18-11-16(6-9-21(18)31)30-38(36,37)17-7-4-15(3)5-8-17/h4-9,11-12,14,20,30H,10,13H2,1-3H3,(H,29,32)(H,34,35)/t20-/m0/s1 |
| InChIKey | SOOLLEBJNGCDOZ-FQEVSTJZSA-N |
| SMILES | CC1=CC=C(C=C1)S(=O)(=O)NC2=CC3=C(C=C2)N(C=C3C(=O)C(F)(F)F)CC(=O)NC(CC(C)C)C(=O)O |
| Reference | [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 |
