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Submit ReviewSR 48692
说明： Selective non-peptide NTS1 antagonist
化学名： 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
纯度： ≥98% (HPLC)
生物活性 for SR 48692
SR 48692 is a neurotensin antagonist; selective for NTS1 over NTS2 (apparent affinity, Ke, is 36 nM for NTS1). Competitively inhibits binding of [125I]-neurotensin to HT29 and N1E115 cell membranes (IC50 values are 15.3 and 20.4 nM respectively). Orally bioavailable.
化合物库 for SR 48692
SR 48692 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for SR 48692
| 分子量 | 587.07 |
| 公式 | C32H31ClN4O5 |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 146362-70-1 |
| PubChem ID | 119192 |
| InChI Key | DYLJVOXRWLXDIG-UHFFFAOYSA-N |
| Smiles | O=C(NC5(C(O)=O)C4CC(CC5C6)CC6C4)C2=NN(C(C3=C(OC)C=CC=C3OC)=C2)C1=C(C=CC(Cl)=C7)C7=NC=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for SR 48692
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 11.74 | 20 |
制备储备液 for SR 48692
以下数据基于产品分子量 587.07。 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.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 8.52 mL | 42.58 mL | 85.17 mL |
| 1 mM | 1.7 mL | 8.52 mL | 17.03 mL |
| 2 mM | 0.85 mL | 4.26 mL | 8.52 mL |
| 10 mM | 0.17 mL | 0.85 mL | 1.7 mL |
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产品说明书 for SR 48692
参考文献 for SR 48692
参考文献是支持产品生物活性的出版物。
Gully et al (1993) Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor. Proc.Natl.Acad.Sci.USA 90 65 PMID: 8380498
Oury-Donat et al (1995) Characterization of the effect of SR48692 on inositol monophosphate, cyclic GMP and cyclic AMP responses linked to neurotensin receptor activation in neuronal and non-neuronal cells. Br.J.Pharmacol. 116 1899 PMID: 8528577
Thomas et al (2009) The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay. Bioorg.Med.Chem.Lett. 19 1438 PMID: 19195889
If you know of a relevant reference for SR 48692, please let us know.
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关键词: SR 48692, SR 48692 supplier, SR48692, neurotensin, nts1, selective, antagonists, Neurotensin, Receptors, 3721, Tocris Bioscience
7 篇 SR 48692 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SR 48692 的部分引用包括：
Deluigi et al (2020) Complexes of the neurotensin receptor 1 with small-molecule ligands reveal structural determinants of full, partial, and inverse agonism. Sci Adv 7 PMID: 33571132
Moody et al (2014) SR48692 inhibits non-small cell lung cancer proliferation in an EGF receptor-dependent manner. PLoS One 100 25 PMID: 24496038
Piccart et al (2015) Neurotensin Induces Presynaptic Depression of D2 DA Autoreceptor-Mediated Neurotransmission in Midbrain DArgic Neurons. J Neurosci 35 11144 PMID: 26245975
Alysandratos et al (2012) Neurotensin and CRH interactions augment human mast cell activation. Life Sci 7 e48934 PMID: 23155429
Rouibi et al (2016) Ventral Midbrain NTS1 Receptors Mediate Conditioned Reward Induced by the Neurotensin Analog, D-Tyr[11]neurotensin. PLoS One 9 470 PMID: 26733785
Bakirtzi et al (2014) The neurotensin-HIF-1α-VEGFα axis orchestrates hypoxia, colonic inflammation, and intestinal angiogenesis. Am J Pathol 184 3405 PMID: 25307345
Toda et al (2014) Maternal separation enhances conditioned fear and decreases the mRNA levels of the neurotensin receptor 1 gene with hypermethylation of this gene in the rat amygdala. PLoS One 9 e97421 PMID: 24831231
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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