ATC 0175 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.
ATC0175 hydrochloride是一种有效的具有口服活性的黑色素浓缩激素受体1(MCH1)选择性拮抗剂,对MCH1的IC50值为13 nM。该物质对5-HT2B和5-HT1A受体也具有亲和性,IC50值分别为9.66 nM和16.9 nM。
黑色素浓缩激素受体1(MCH1)是G蛋白偶联受体家族的成员[1],是一种整合血浆膜蛋白,可结合黑色素浓缩激素。该蛋白可抑制cAMP积累,并可刺激胞内钙流,可能参与食物消耗的神经调控。
在体外,试验表明该物质是一种有效的对MCH1R具有高亲和性的拮抗剂。受体结合和功能试验(MCH诱导的[Ca2+]升高)表明ATC0175是一种非竞争性的MCH1R拮抗剂[1]。
在体内,ATC0175在包括社会交往试验、高架十字迷宫试验、母婴分离引起的发声和应激性体温过高在内的多种动物焦虑模型中具有抗焦虑作用。此外,ATC0175疗法在强迫游泳试验中也具有抗抑郁作用[2]。
参考文献:
1. Semple G, Tran TA, Kramer B, et al. Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation. Bioorganic & medicinal chemistry letters. 2009;19(21):6166-6171.
2. Chaki S, Yamaguchi J, Yamada H, et al. ATC0175: an orally active melanin-concentrating hormone receptor 1 antagonist for the potential treatment of depression and anxiety. CNS drug reviews. 2005;11(4):341-352.
Physical Appearance | Off-white solid |
Storage | Store at -20°C |
M.Wt | 461.94 |
Cas No. | 510733-97-8 |
Formula | C23H25F2N5O·HCl |
Solubility | insoluble in DMSO; <11.55mg/ml in ethanol |
Chemical Name | N-((1s,4s)-4-((4-(dimethylamino)quinazolin-2-yl)amino)cyclohexyl)-3,4-difluorobenzamide hydrochloride |
SDF | Download SDF |
Canonical SMILES | FC1=CC(C(N[C@H]2CC[C@H](CC2)NC3=NC4=CC=CC=C4C(N(C)C)=N3)=O)=CC=C1F.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。 |