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Documenti

SML0278

Sigma-Aldrich

SR 48692

≥98% (HPLC)

Sinonimo/i:

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

Formula empirica (notazione di Hill):
C32H31ClN4O5
Numero CAS:
146362-70-1
Peso molecolare:
587.07
Codice UNSPSC:
12352200
ID PubChem:
329825286
NACRES:
NA.77

Saggio

≥98% (HPLC)

Forma fisica

powder

Colore

white to beige

Solubilità

DMSO: ≥2 mg/mL (warmed)

Temperatura di conservazione

−20°C

Stringa SMILE

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)
DYLJVOXRWLXDIG-UHFFFAOYSA-N

Informazioni sul gene

human ... NTSR1(4923)

Applicazioni

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

Azioni biochim/fisiol

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.

Caratteristiche e vantaggi

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.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

Cerca il Certificati d'analisi (COA) digitando il numero di lotto/batch corrispondente. I numeri di lotto o di batch sono stampati sull'etichetta dei prodotti dopo la parola ‘Lotto’ o ‘Batch’.

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Nicholas C K Valerie et al.
Cancer research, 71(21), 6817-6826 (2011-09-10)
Radiotherapy combined with androgen depletion is generally successful for treating locally advanced prostate cancer. However, radioresistance that contributes to recurrence remains a major therapeutic problem in many patients. In this study, we define the high-affinity neurotensin receptor 1 (NTR1) as
Fabiana G Costa et al.
Neuropeptides, 41(2), 83-91 (2007-02-06)
Psychostimulant-induced locomotor sensitization has been related to changes within the mesolimbic dopamine system and has been suggested to be useful to study mechanisms underlying drug craving. Neurotensin is a neuropeptide co-localized with dopamine in the mesolimbic system. The response to
Polina Petkova-Kirova et al.
Brain research bulletin, 77(2-3), 129-135 (2008-08-30)
The effects of the peptide transmitter neurotensin (NT) on the release of acetylcholine (ACh), gamma-aminobutyric acid (GABA), glutamate (Glu), aspartate (Asp), and taurine from the prefrontal cortex (PFC) of freely moving rats were studied by transversal microdialysis. Neurotensin (0.2 and
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
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
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