ADX 10059 hydrochloride
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.
ADX 10059 hydrochloride是mGlu5受体的有效选择性负向变构调节剂,IC50值为17.1 nM [1]。
代谢型谷氨酸受体5(mGlu5受体)是G蛋白偶联受体,是一种谷氨酸受体,谷氨酸是参与中枢神经系统信号传导的主要神经递质[2]。
ADX 10059 hydrochloride是mGlu5受体的有效选择性负向变构调节剂。在偏头痛患者中,ADX 10059引起16.1%的患者无疼痛反应,对照组仅为4.5%[1]。对胃食管反流病(GORD)患者进行24小时的食管pH监测,250 mg 的ADX10059将pH < 4的酸暴露时间的百分比从7.2%显著降低到3.6%。此外,ADX 10059显著降低症状反流发作的持续时间和数量,并减少食管酸暴露 [2]。
参考文献:
[1]. Marin JC, Goadsby PJ. Glutamatergic fine tuning with ADX-10059: a novel therapeutic approach for migraine? Expert Opin Investig Drugs, 2010, 19(4): 555-561.
[2]. Keywood C, Wakefield M, Tack J. A proof-of-concept study evaluating the effect of ADX10059, a metabotropic glutamate receptor-5 negative allosteric modulator, on acid exposure and symptoms in gastro-oesophageal reflux disease. Gut, 2009, 58(9): 1192-1199.
Physical Appearance | Yellow solid |
Storage | Desiccate at RT |
M.Wt | 276.74 |
Cas No. | 757949-98-7 |
Formula | C15H13FN2·HCl |
Solubility | <6.92mg/ml in H2O; <27.67mg/ml in DMSO |
Chemical Name | 2-((3-fluorophenyl)ethynyl)-4,6-dimethylpyridin-3-amine hydrochloride |
SDF | Download SDF |
Canonical SMILES | CC1=CC(C)=NC(C#CC2=CC(F)=CC=C2)=C1N.Cl |
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。 |