WAY-100635
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
5-HT1A受体介导各种血清素功能,可能与各种病症有关,包括抑郁和焦虑症\阿尔茨海默病及精神分裂症.WAY-100635是一种潜在的5-HT1A 受体的SPECT配体.
体外实验:WAY-100635取代5-HT1A放射配体[3H]8-OH-DPAT与大鼠海马膜的特异结合,pIC50值为8.87.在功能试验中,WAY-100635是强效的5-HT1A受体拮抗剂,还没有证据证明任何5-HT1A受体激动剂或部分激动剂的活性.在离体豚鼠回肠中,WAY-100635是5-carboxamidotryptamine的5-HT1A受体激动效应的有效的和难以逾越的拮抗剂,0.3 nM 浓度下pA 2值为9.71[2].
体内实验:在麻醉大鼠中,WAY-100635在本身没有抑制作用的剂量下阻断8-OH-DPAT对中缝背核神经元放电的抑制作用.在行为模型中,WAY-100635不诱发明显行为改变,但是在大鼠和豚鼠中,强效拮抗由8-OH-DPAT诱发的行为综合征(最小有效量和ID50值分别为0.003 mg/kg s.c和0.01 mg/kg s.c.).在小鼠和大鼠中,WAY-100635也阻滞由8-OH-DPAT诱发的低体温症,ID50值为0.01 mg/kg s.c. [2].
临床实验:使用配体[11C]-WAY100635\开放标记和非随机的正电子发射断层扫描研究对健康男性受试者进行研究,探讨GSK163090单次口服剂量的脑内5-HT1A受体占有率\药代动力学及安全性.
参考文献：
[1] Al Hussainy R, Verbeek J, van der Born D, Braker AH, Leysen JE, Knol RJ, Booij J, Herscheid JK. Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A receptor. J Med Chem. 2011;54(10):3480-91.
[2] Forster EA, Cliffe IA, Bill DJ, Dover GM, Jones D, Reilly Y, Fletcher A. A pharmacological profile of the selective silent 5-HT1A receptor antagonist, WAY-100635. Eur J Pharmacol. 1995;281(1):81-8.
| Storage | Store at -20°C |
| M.Wt | 422.56 |
| Cas No. | 162760-96-5 |
| Formula | C25H34N4O2 |
| Synonyms | WAY 100635; WAY100635 |
| Solubility | ≥42.3 mg/mL in DMSO; insoluble in H2O; ≥134.2 mg/mL in EtOH |
| Chemical Name | N-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-pyridin-2-ylcyclohexanecarboxamide |
| SDF | Download SDF |
| Canonical SMILES | COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | WAY-100635是一种强效的和沉默的血清素5-HT1A受体拮抗剂,IC50值为2.2 nM. | |||||
| 靶点 | 5-HT1A receptor | |||||
| IC50 | 2.2 nM | |||||
质量控制和MSDS
- 批次:
化学结构
