NTRC-824 | CAS#1623002-61-8 | NTS receptor antagonist

MedKoo Cat#: 563469 | Name: NTRC-824

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

NTRC-824 is a potent and selective non-peptide neurotensin (NTS) type-2 receptor antagonist.

Chemical Structure

NTRC-824

CAS#1623002-61-8

Theoretical Analysis

MedKoo Cat#: 563469

Name: NTRC-824

CAS#: 1623002-61-8

Chemical Formula: C25H26F3N3O6S

Exact Mass: 553.1494

Molecular Weight: 553.55

Elemental Analysis: C, 54.25; H, 4.73; F, 10.30; N, 7.59; O, 17.34; S, 5.79

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 440.00	2 Weeks
50mg	USD 1,545.00	2 Weeks

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Related CAS #

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Synonym

NTRC-824; NTRC 824; NTRC824;

IUPAC/Chemical Name

(2-(5-((4-methylphenyl)sulfonamido)-3-(2,2,2-trifluoroacetyl)-1H-indol-1-yl)acetyl)-L-leucine

InChi Key

SOOLLEBJNGCDOZ-FQEVSTJZSA-N

InChi Code

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

SMILES Code

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

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.03.00

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

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.

In vitro activity:

To identify novel NTS2 selective analgesics, this study searched for NTS2 selective nonpeptide compounds using a FLIPR assay and identified the title compound (NTRC-824, 5) that, to this study’s knowledge, is the first nonpeptide that is selective for NTS2 versus NTS1 and behaves like the endogenous ligand neurotensin in the functional assay. Reference: J Med Chem. 2014 Sep 11;57(17):7472-7. https://pubmed.ncbi.nlm.nih.gov/25157640/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO	38.1	68.81
	Ethanol	55.4	100.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 553.55 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

Thomas JB, Giddings AM, Wiethe RW, Olepu S, Warner KR, Sarret P, Gendron L, Longpre JM, Zhang Y, Runyon SP, Gilmour BP. 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. doi: 10.1021/jm500857r. Epub 2014 Aug 26. PMID: 25157640; PMCID: PMC4161155.

In vitro protocol:

In vivo protocol:

TBD

1: Thomas JB, Giddings AM, Wiethe RW, Olepu S, Warner KR, Sarret P, Gendron L, Longpre JM, Zhang Y, Runyon SP, Gilmour BP. 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. doi: 10.1021/jm500857r. Epub 2014 Aug 26. PubMed PMID: 25157640; PubMed Central PMCID: PMC4161155.