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SML0278

SR 48692

Name: SR 48692
Brand: SIGMA

≥98% (HPLC), nonpeptide NT1 neurotensin receptor antagonist , powder

Synonym(s):

2-[[[1-(7-Chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]-tricyclo[3.3.1.13,7]decane-2-carboxylic acid, Meclinertant

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About This Item

Empirical Formula (Hill Notation):

C₃₂H₃₁ClN₄O₅

CAS Number:

146362-70-1

Molecular Weight:

587.07

UNSPSC Code:

12352200

PubChem Substance ID:

329825286

NACRES:

NA.77

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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Product Name

SR 48692, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: ≥2 mg/mL (warmed)

storage temp.

−20°C

SMILES string

COc1cccc(OC)c1-c2cc(nn2-c3ccnc4cc(Cl)ccc34)C(=O)NC5(C6CC7CC(C6)CC5C7)C(O)=O

InChI

1S/C32H31ClN4O5/c1-41-27-4-3-5-28(42-2)29(27)26-16-24(36-37(26)25-8-9-34-23-15-21(33)6-7-22(23)25)30(38)35-32(31(39)40)19-11-17-10-18(13-19)14-20(32)12-17/h3-9,15-20H,10-14H2,1-2H3,(H,35,38)(H,39,40)

InChI key

DYLJVOXRWLXDIG-UHFFFAOYSA-N

Gene Information

human ... NTSR1(4923)

Related Categories

Bioactive Small Molecules

Application

SR 48692 has been used as a neurotensin high-affinity receptor 1 (NTSR1) antagonist:

to explore the function of NTSR1 in glioblastoma (GBM) cells
to determine the roles of neurotensin (NT) in the regulation of bile acid (BA) uptake, in vivo
to explore the involvement of NTSR1 versus NTSR2 in mice

Biochem/physiol Actions

SR 48692 is a high affinity, orally bioavailable and selective nonpeptide NT1 neurotensin receptor antagonist that antagonizes neurotensin-induced calcium mobilization with a pA2 of 8.13 in HT-29 human colon carcinoma cell line, and blocks the ability of neurotensin to increase GABA levels in the prefrontal cortex.

SR 48692 is a high affinity, orally bioavailable and selective nonpeptide NT1 neurotensin receptor antagonist.

Features and Benefits

This compound is featured on the Neurotensin Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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The role of neurotensin in passive avoidance learning in the rat central nucleus of amygdala.

Kristóf László et al.

Behavioural brain research, 226(2), 597-600 (2011-09-29)

Tridecapeptide neurotensin (NT) acts as a neurotransmitter and/or neuromodulator and plays a role in learning and reinforcement. The central nucleus of amygdala (CeA), which is relatively rich in NT and neurotensin-1 receptors (NTS1), participates in the regulation of memory and

The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay.

James B Thomas et al.

Bioorganic & medicinal chemistry letters, 19(5), 1438-1441 (2009-02-07)

In a search for nonpeptide agonists for the neurotensin receptor (NTR1), we replaced the adamantyl amino acid moiety found in the antagonist SR48692 (1a) with leucine and related alpha-alkylamino acids found in peptide agonists. When tested in a calcium mobilization

Bidirectional regulation of dopamine D2 and neurotensin NTS1 receptors in dopamine neurons.

C Jomphe et al.

The European journal of neuroscience, 24(10), 2789-2800 (2006-11-23)

Several lines of evidence suggest a close association between dopamine (DA) and neurotensin (NT) systems in the CNS. Indeed, in the rodent brain, abundant NT-containing fibres are found in DA-rich areas such as the ventral tegmental area and substantia nigra.

The role of neurotensin in positive reinforcement in the rat central nucleus of amygdala.

Kristóf László et al.

Behavioural brain research, 208(2), 430-435 (2009-12-29)

In the central nervous system neurotensin (NT) acts as a neurotransmitter and neuromodulator. It was shown that NT has positive reinforcing effects after its direct microinjection into the ventral tegmental area. The central nucleus of amygdala (CeA), part of the

Neurotensin receptor 1 signaling promotes pancreatic cancer progression.

Kei Takahashi et al.

Molecular oncology, 15(1), 151-166 (2020-10-10)

Pancreatic cancer is one of the cancers with the poorest prognosis, with a 5-year survival rate of approximately 5-10%. Thus, it is urgent to identify molecular targets for the treatment of pancreatic cancer. Using serial transplantations in a mouse pancreatic

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Global Trade Item Number

SKU	GTIN
SML0278-25MG	04061832899602
SML0278-5MG	04061832899619

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