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Submit ReviewTCS 1102
说明： Potent, dual orexin receptor antagonist
化学名： N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide
纯度： ≥98% (HPLC)
生物活性 for TCS 1102
TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively). Inhibits ADL-orexin B-mediated locomotion following i.p. administration in vivo and blocks orexin-A (Cat.No.1455) mediated increases in feeding behaviour. Brain penetrant.
许可信息
Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans)
技术数据 for TCS 1102
| 分子量 | 470.59 |
| 公式 | C27H26N4O2S |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 916141-36-1 |
| PubChem ID | 11960895 |
| InChI Key | YSBGRVXJEMSEQY-DEOSSOPVSA-N |
| Smiles | O=C(CSC2=NC(C=CC=C5)=C5N2C)N1CCC[C@H]1[C@](NC3=CC=CC=C3C4=CC=CC=C4)=O |
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 TCS 1102
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 47.06 | 100 | |
| ethanol | 47.06 | 100 |
制备储备液 for TCS 1102
以下数据基于产品分子量 470.59。 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 |
|---|---|---|---|
| 1 mM | 2.12 mL | 10.62 mL | 21.25 mL |
| 5 mM | 0.42 mL | 2.12 mL | 4.25 mL |
| 10 mM | 0.21 mL | 1.06 mL | 2.12 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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产品说明书 for TCS 1102
参考文献 for TCS 1102
参考文献是支持产品生物活性的出版物。
Winrow et al (2010) Orexin receptor antagonism prevents transcriptional and behavioral plasticity resulting from stimulant exposure. Neuropharmacology 58 185 PMID: 19596018
Bergman et al (2008) Proline bis-amides as potent dual orexin receptor antagonists. Bioorg.Med.Chem.Letts 18 1425
Khoo et al (2017) The dual orexin receptor antagonist TCS1102 does not affect reinstatement of nicotine-seeking. PLoS One 12 e0173967 PMID: 28296947
If you know of a relevant reference for TCS 1102, please let us know.
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关键词: TCS 1102, TCS 1102 supplier, TCS1102, orexin, receptors, OX1, OX2, antagonists, non-selective, dual, potent, merck, Non-selective, Orexin, 3818, Tocris Bioscience
7 篇 TCS 1102 的引用文献
引用文献是使用了 Tocris 产品的出版物。 TCS 1102 的部分引用包括：
Yu et al (2023) Circadian regulation of developmental synaptogenesis via the hypocretinergic system. Nat Commun 14 3195 PMID: 37268623
Daniel J et al (2021) Orexin Modulation of VTA Dopamine Neuron Activity: Relevance to Schizophrenia. Int J Neuropsychopharmacol 24 344-353 PMID: 33587746
Khoo et al (2017) The dual orexin receptor antagonist TCS1102 does not affect reinstatement of nicotine-seeking. PLoS One PMID: 28296947
Mavanji et al (2015) Promotion of Wakefulness and Energy Expenditure by Orexin-A in the Ventrolateral Preoptic Area. Sleep 38 1361 PMID: 25845696
Dong et al (2015) Blocking of orexin receptors in the paraventricular nucleus of the thalamus has no effect on the expression of conditioned fear in rats. Front Behav Neurosci 9 161 PMID: 26136671
Putula et al (2014) Calcium affects OX1 orexin (hypocretin) receptor responses by modifying both orexin binding and the signal transduction machinery. Br J Pharmacol 171 5816 PMID: 25132134
Korim et al (2014) Orexinergic activation of medullary premotor neurons modulates the adrenal sympathoexcitation to hypothalamic glucoprivation. Diabetes 63 1895 PMID: 24550189
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*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.