跳转至内容
Merck
所有图片(1)

主要文件

查看所有文档

SML2117

Sigma-Aldrich

TCS-1102

≥98% (HPLC)

别名:

BBAC, (2S)-N-[1,1′-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl]-2-pyrrolidinecarboxamide, DORA-1, N-(1,1′-Biphenyl-2-yl)-1-{[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl}-L-prolinamide, TCS 1102, TCS1102, (2S)-N-[1,1′-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl]-2-pyrrolidinecarboxamide

登录查看公司和协议定价
所有图片(1)

About This Item

经验公式（希尔记法）:
C27H26N4O2S
CAS号:
916141-36-1
分子量:
470.59
MDL號碼:
MFCD18086894
分類程式碼代碼:
12352200

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

CN1C2=CC=CC=C2N=C1SCC(N3CCC[C@H]3C(NC4=CC=CC=C4C5=CC=CC=C5)=O)=O

InChI

1S/C27H26N4O2S/c1-30-23-15-8-7-14-22(23)29-27(30)34-18-25(32)31-17-9-16-24(31)26(33)28-21-13-6-5-12-20(21)19-10-3-2-4-11-19/h2-8,10-15,24H,9,16-18H2,1H3,(H,28,33)/t24-/m0/s1

InChI 密鑰

YSBGRVXJEMSEQY-DEOSSOPVSA-N

正在寻找类似产品? 访问 产品对比指南

生化／生理作用

TCS-1102 (DORA-1) is a high-affinity (Ki = 3 nM against [3H]-TCS-1102 for binding hOX1R and Ki = 0.2 nM against [3H]-pyrrolylphenyl analog for binding hOX2R) dual orexin receptor antagonist (DORA) that potently inhibits calcium mobilization in hOX1R & hOX2R CHO transfectants (IC50 = 17 & 4 nM, respectively). TCS-1102 promotes sleep (50-100 mg/kg p.o.), decreases fear/anxiety (10-20 mg/kg i.p.), and inhibits ADL-orexin B peptide-induced locomotion (by 56%/74%/100% with 15/50/100 mg/kg i.p. 30 min before ADL-XB ICV injection) with good pharmacokinetic properties, brain penetration (Brain/plasma conc. = 2.37 μM/3.50 μM 3 hrs post 100 mg/kg i.p.), and oral availability (Cmax/AUC(0–24h) = 1.21 μM/6.8 μM h and 3.01 μM/12.5 μM h, respectively post 50 and 100 mg/kg p.o. dosage) in rats in vivo.

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

It looks like we've run into a problem, but you can still download Certificates of Analysis from our 文件 section.

如需帮助，请联系 客户支持

已有该产品？

在文件库中查找您最近购买产品的文档。

访问文档库

Jyrki P Kukkonen
Cellular signalling, 28(2), 51-60 (2015-11-20)
There are two subtypes of orexin receptors, OX1 and OX2. Signalling pathways have been mapped in much higher detail for OX1 receptors than OX2 receptors. Almost all the detailed studies have been performed in Chinese hamster ovary cells, and we
Guan-Ling Lu et al.
Neuropharmacology, 107, 168-180 (2016-03-12)
The orexin system consists of two peptides, orexin A and B and two receptors, OX1R and OX2R. It is implicated in learning and memory regulation while controversy remains on its role in modulating hippocampal synaptic plasticity in vivo and in vitro. Here
Yuhei Nishimura et al.
Frontiers in pharmacology, 6, 257-257 (2015-11-19)
Sleep-wake states are impaired in various neurological disorders. Impairment of sleep-wake states can be an early condition that exacerbates these disorders. Therefore, treating sleep-wake dysfunction may prevent or slow the development of these diseases. Although many gene products are likely
Jeffrey M Bergman et al.
Bioorganic & medicinal chemistry letters, 18(4), 1425-1430 (2008-01-22)
A series of OX(2)R/OX(1)R dual orexin antagonists was prepared based on a proline bis-amide identified as a screening lead. Through a combination of classical and library synthesis, potency enhancing replacements for both amide portions were discovered. N-methylation of the benzimidazole
Xiaoyu Chen et al.
Brain structure & function, 219(6), 2103-2118 (2013-08-21)
Orexins (hypocretins) are peptides that have been shown to regulate behavioral arousal and wakefulness. Recent evidence indicates that orexin neurons are activated by stress and that orexins play a role in anxiety. The present paper describes a series of experiments
查看所有相关文献

我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.

联系技术服务部门