LY2119620
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.
LY2119620是M2/M4受体的选择性正向别构调节剂[1].
毒蕈碱乙酰胆碱受体(M1-M5)是调控神经递质Ach功能的G蛋白偶联受体,在平滑肌控制\外分泌腺功能\情绪和认知中扮演重要角色[1].
LY2119620是一种选择性的M2/M4受体正向别构调节剂,在[35S]GTPγS结合实验中,LY2119620具有适度的别构激动活性,对M2和M4受体分别为23.2%和16.8%.LY2119620和ACh结合可引起对M4受体和M2受体的协同因子α值分别为79.4和19.5.LY2119620和正位激动剂(Iperoxo或Oxo-M)也具有协同性[1].M2受体可同时结合LY2119620和iperoxo.LY2119620与反相激动剂NMS具有温和的负协同性,与iperoxo具有强烈的正协同性.当[3H]LY2119620与mAChR协同结合时,LY2119620可显著提高Bmax值而不改变Kd,表明其为G蛋白依赖过程[3].
参考文献：
[1]. Croy CH, Schober DA, Xiao H, et al. Characterization of the novel positive allosteric modulator, LY2119620, at the muscarinic M(2) and M(4) receptors. Mol Pharmacol, 2014, 86(1): 106-115.
[2]. Kruse AC, Ring AM, Manglik A, et al. Activation and allosteric modulation of a muscarinic acetylcholine receptor. Nature, 2013, 504(7478): 101-106.
[3]. Schober DA, Croy CH, Xiao H, et al. Development of a radioligand, [(3)H]LY2119620, to probe the human M(2) and M(4) muscarinic receptor allosteric binding sites. Mol Pharmacol, 2014, 86(1): 116-123.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 437.94 |
| Cas No. | 886047-22-9 |
| Formula | C19H24ClN5O3S |
| Solubility | ≥21.9 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | 3-amino-5-chloro-N-cyclopropyl-4-methyl-6-[2-(4-methylpiperazin-1-yl)-2-oxoethoxy]thieno[2,3-b]pyridine-2-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=C2C(=C(SC2=NC(=C1Cl)OCC(=O)N3CCN(CC3)C)C(=O)NC4CC4)N |
| 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。 |
化学结构
