A-740003
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.
A-740003是P2X7受体的一个选择性和竞争性的拮抗剂,对老鼠和人类P2X7受体的IC50值分别为18 nM和40 nM[1]。
P2X7受体是ATP-敏感性离子型P2X受体家族(P2X1-P2X7)的成员。P2X7受体在免疫性的遗传细胞中可以引发各种反应,如caspase的激活、细胞因子释放、膜穿透、细胞凋亡和细胞增殖[1]。
激活的P2X7受体可以迅速改变胞内钙离子浓度、释放白介素1β(IL-1β)和细胞质膜孔隙形成。在具有巨噬细胞表型的人类THP-1细胞中P2X7受体表达、IL-1β释放和孔隙的形成是由于P2X7受体的激活。A-740003有效地抑制了孔隙形成(用Yo-Pro吸收法测量,IC50值92 nM),阻止了IL-1β的释放(IC50值156 nM)[1]。
参考文献:
[1]. Prisca Honore, Diana Donnelly-Roberts, Marian T. Namovic, et al. A-740003 [N-(1-{[(Cyanoimino)(5-quinolinylamino)methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a Novel and Selective P2X7 Receptor Antagonist, Dose-Dependently Reduces Neuropathic Pain in the Rat. Journal of Pharmacology and Experimental Therapeutics, 2006, 319:1376-1385.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 474.57 |
Cas No. | 861393-28-4 |
Formula | C26H30N6O3 |
Synonyms | A 740003;A740003 |
Solubility | ≥23.73 mg/mL in DMSO; insoluble in H2O; ≥2.48 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | N-[1-[(E)-[(cyanoamino)-(quinolin-5-ylamino)methylidene]amino]-2,2-dimethylpropyl]-2-(3,4-dimethoxyphenyl)acetamide |
SDF | Download SDF |
Canonical SMILES | CC(C)(C)C(NC(=O)CC1=CC(=C(C=C1)OC)OC)N=C(NC#N)NC2=CC=CC3=C2C=CC=N3 |
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。 |
描述 | A-740003是P2X7受体有效的、选择性和竞争性的拮抗剂,对老鼠和人类P2X7受体的IC50值分别为18 nM和40 nM。 | |||||
靶点 | P2X7 receptor | |||||
IC50 | 18 nM (rat) 40 nM (human) |
质量控制和MSDS
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