| Bioactivity | 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]. | |||||||||
| Target | IC50: 38 nM (Nurotensin receptor type 2)Ki: 202 nM (Nurotensin receptor type 2) | |||||||||
| Invitro | 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]. | |||||||||
| Name | NTRC-824 | |||||||||
| CAS | 1623002-61-8 | |||||||||
| Formula | C25H26F3N3O6S | |||||||||
| Molar Mass | 553.55 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| 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 |
NTRC-824
CAS: 1623002-61-8 F: C25H26F3N3O6S W: 553.55
NTRC-824 (Compound 5) is a potent, selective and neurotensin-like nonpeptide neurotensin receptor type 2 (NTS2) antagoni
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