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모든 사진(1)

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SML0278

Sigma-Aldrich

SR 48692

≥98% (HPLC)

동의어(들):

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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모든 사진(1)

About This Item

실험식(Hill 표기법):
C32H31ClN4O5
CAS Number:
146362-70-1
Molecular Weight:
587.07
UNSPSC 코드:
12352200
PubChem Substance ID:
329825286
NACRES:
NA.77

분석

≥98% (HPLC)

형태

powder

색상

white to beige

solubility

DMSO: ≥2 mg/mL (warmed)

저장 온도

−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

유전자 정보

human ... NTSR1(4923)

애플리케이션

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

생화학적/생리학적 작용

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.

특징 및 장점

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 Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

시험 성적서(COA)

제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.

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문서 라이브러리 방문

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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