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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Temanogrel
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
887936-68-7
- 规格：
1mg/5mg/10mg/25mg
| 规格： | 1mg | 产品价格： | ￥610.0 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ￥1280.0 |
| 规格： | 10mg | 产品价格： | ￥2060.0 |
| 规格： | 25mg | 产品价格： | ￥3700.0 |
| 基本信息 | |
| CAS | No.887936-68-7 |
| 英文名称 | Temanogrel |
| 分子式 | C24H28N4O4 |
| 分子量 | 436.5 |
| 溶解性 | Soluble in DMSO ≥10mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| SMILES | CN1C(=CC=N1)C2=C(C=CC(=C2)NC(=O)C3=CC(=CC=C3)OC)OCCN4CCOCC4 |
| InChIKey | ZEOQUKRCASTCFR-UHFFFAOYSA-N |
| InChI | InChI=1S/C24H28N4O4/c1-27-22(8-9-25-27)21-17-19(26-24(29)18-4-3-5-20(16-18)30-2)6-7-23(21)32-15-12-28-10-13-31-14-11-28/h3-9，16-17H，10-15H2，1-2H3，(H，26，29) |
| PubChem CID | 11604525 |
| 靶点 | 5-HT Receptor |
| 通路 | Neuronal Signaling;GPCR & G Protein |
| 背景说明 | Temanogrel 是一个高选择性的 5-HT2A 受体拮抗剂。 |
| 生物活性 | Temanogrel is a highly selective 5-HT2A receptor antagonist with a Ki of 4.9 nM.[1-3] |
| In Vitro | Temanogrel is a highly selective 5-HT2A receptor antagonist with a Ki of 4.9 nM. Temanogrel inhibits inositol phosphate accumulation with an IC50 of 5.2 nM. Temanogrel exhibits potent inhibition of serotonin mediated amplification of ADP-stimulated human and dog platelet aggregation (IC50=8.7 and 23.1 nM， respectively)[1]. Pretreatment of aortic rings with Temanogrel prevents the vasoconstriction caused by 20 μM 5-HT in a concentration-dependent manner. Preincubation with Temanogrel also significantly inhibits the 5-HT-stimulated DNA synthesis with an IC50 of 13±7 nM[3]. |
| 细胞实验 | There are no differences in heart rate or mean arterial pressure between saline-treated and Temanogrel-treated groups at any time during the experiment (that is， for mean arterial pressure， P=0.508 between groups， and P=0.540 for group-time interaction). In dogs assigned to receive Temanogrel， plasma Temanogrel levels show a rapid and sustained increase， averaging 25.5±4.1， 28.7±4.6 and 31.2±4.5 ng/mL， respectively， at 10 min， 1.25 h and 2.25 h after the start of treatment[3]. |
| 细胞实验 | To provide further insights into the effect of Temanogrel on platelet-dependent clot formation in models devoid of vascular smooth muscle， two in vitro post hoc experiments are performed. Paired aliquots of heparinized whole blood are incubated with Temanogrel (100 nM) or vehicle for 10 min at 37°C， and then placed in a thromboelastogram (TEG) pin-and-cup system with 10 μm serotonin， reptilase， and activated factor XIII (n=3 paired samples). The maximum amplitude of torsion is quantified for all samples. Aliquots of citrated blood (n=3 pairs) are incubated with Temanogrel (100 nM) or vehicle for 10 min at 37°C， and then pipetted into collagen-ADP cartridges. For each sample， the time (in seconds) required for the complete platelet-mediated thrombotic occlusion of the membrane aperture is recorded[2]. |
| 动物实验 | Adult male beagle dogs (n=3) are used and receive a single oral gavage dose of Temanogrel at 10 mg/kg. Temanogrel is formulated in sterile water at 5 mL/kg. Animals are fasted before Temanogrel delivery. Serial sampling is used to obtain plasma concentration versus time profiles. Whole blood samples are collected via jugular vein venipuncture over a 24-h period. Plasma is prepared by centrifugation from sodium heparin-treated whole blood， frozen， and stored at approximately -20°C until bioanalytical analysis[3]. |
| 数据来源文献 | [1]. Xiong Y， et al. Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thr [2]. Przyklenk K， et al. Targeted inhibition of the serotonin 5HT2A receptor improves coronary patency in an in vivo model of recurrent thrombosis. J Thromb Haemost. 2010 Feb;8(2):331-40. [3]. Adams JW， et al. APD791， 3-methoxy-n-(3-(1-methyl-1h-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide， a novel 5-hydroxytryptamine 2A receptor antagonist: pharmacological profile， pharmacokinetics， platelet activity and vascular biology. J Pharmacol E |
| 单位 | 瓶 |
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文献和实验大鼠 神经肽Y （NP-Y ） 酶联免疫分析（ ELISA ） 试剂盒使用说明书 本试剂仅供研究使用 目的：本试剂盒用于测定大鼠血清，血浆及相关液体样本中 神经肽Y （NP-Y ） 的 含量。 实验原理： 本试剂盒应用双抗体夹心法测定标本中大鼠 神经肽 Y （ NP-Y ） 水平。用纯化的大鼠 神经肽 Y （ NP-Y ） 抗体包被微孔板，制成固相抗体，往包被单抗的微孔中依次加入 神经肽 Y （ NP
作用最强，特异性也较高。假性胆碱酯酶也叫丁酰胆碱酯酶（BuChE）、血清胆碱酯酶，广泛存在于神经胶质细胞、血浆、肝、肾、肠中，主要由肝细胞制造。对Ach的特异性较低，假性胆碱酯酶可水解其他胆碱酯类，如琥珀胆碱。在肝病的治疗中，关注胆碱酯酶主要是假性假性胆碱酯酶，是个很重要的指标，反应的是肝脏的代偿应激能力。在肝功能损伤程度参考指标中，胆碱酯酶反应的意义：大于等于5400 U/L轻度损伤，4500-5400 U/L中度损伤，小于等于4500 U/L重度损伤。
录了来自5400种不同物种的300万条核酸序列和560万条蛋白质序列。用户可以通过Entrez核酸和蛋白质数据库搜索到RefSeq序列，也可以通过NCBI FTP站点进入RefSeq数据库。 5.1.5 GenBank和其它数据库来源的序列 用户可以通过三个Entrez数据库——Nucleotide、EST和Genome Survey Sequence(GSS)(这三个数据库在E-Utilities中分别称作nuccore、nucest和nucgss)搜索到GenBank中
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