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Submit ReviewMRS 2500 tetraammonium salt
说明： Highly potent and selective P2Y1 antagonist
化学名： (1R*,2S*)-4-[2-Iodo-6-(methylamino)-9H-purin-9-yl]-2-(phosphonooxy)bicyclo[3.1.0]hexane-1-methanol dihydrogen phosphate ester tetraammonium salt
纯度： ≥96% (HPLC)
生物活性 for MRS 2500 tetraammonium salt
MRS 2500 tetraammonium salt is a highly potent and selective antagonist of the platelet P2Y1 receptor (Ki = 0.78 nM). Inhibits ADP-induced aggregation of human platelets with an IC50 value of 0.95 nM. Inhibits the upregulation of NTPDase1 by ATPγS. Prevents thrombus formation in vivo.
许可信息
Sold under license from the NIH, US Patent 10/169975
技术数据 for MRS 2500 tetraammonium salt
| 分子量 | 629.29 |
| 公式 | C13H18N5O8P2I.4NH3 |
| 储存 | Store at -20°C |
| 纯度 | ≥96% (HPLC) |
| CAS Number | 630103-23-0 |
| PubChem ID | 90488745 |
| InChI Key | FVTFHHDVLNQSME-AVAGOIHISA-N |
| Smiles | IC4=NC1=C(C(NC)=N4)N=CN1[C@H]2C[C@H](OP(O)(O)=O)[C@@]3(COP(O)(O)=O)[C@@H]2C3.N.N.N.N |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for MRS 2500 tetraammonium salt
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 12.59 | 20 |
制备储备液 for MRS 2500 tetraammonium salt
以下数据基于产品分子量 629.29。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 7.95 mL | 39.73 mL | 79.45 mL |
| 1 mM | 1.59 mL | 7.95 mL | 15.89 mL |
| 2 mM | 0.79 mL | 3.97 mL | 7.95 mL |
| 10 mM | 0.16 mL | 0.79 mL | 1.59 mL |
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产品说明书 for MRS 2500 tetraammonium salt
参考文献 for MRS 2500 tetraammonium salt
参考文献是支持产品生物活性的出版物。
Kim et al (2003) 2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists. J.Med.Chem 46 4974 PMID: 14584948
Cattaneo et al (2004) Antiaggregatory activity in human platelets of potent antagonists of the P2Y1 receptor. Biochem.Pharmacol. 68 1995 PMID: 15476670
Hechler et al (2006) MRS2500 [2-iodo-N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3', 5'-bisphosphate], a potent, selective, and stable antagonist of the platelet P2Y1 receptor with strong antithrombotic activity in mice. J.Pharmacol.Exp.Ther. 316 556 PMID: 16236815
Lu et al (2007) Stimulation of the P2Y1 receptor up-regulates nucleoside-triphosphate diphosphohydrolase-1 in human retinal pigment epithelial cells. J.Pharmacol.Exp.Ther. 323 157 PMID: 17626796
If you know of a relevant reference for MRS 2500 tetraammonium salt, please let us know.
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22 篇 MRS 2500 tetraammonium salt 的引用文献
引用文献是使用了 Tocris 产品的出版物。 MRS 2500 tetraammonium salt 的部分引用包括：
Gao et al (2013) The role of P2Y(14) and other P2Y receptors in degranulation of human LAD2 mast cells. J Pharmacol Exp Ther 9 31 PMID: 22825617
Hwang et al (2011) β-nicotinamide adenine dinucleotide is an enteric inhibitory neurotransmitter in human and nonhuman primate colons. Gastroenterology 140 608 PMID: 20875415
Högberg et al (2009) Mild hypothermia does not attenuate platelet aggregation and may even increase ADP-stimulated platelet aggregation after clopid. treatment. Purinergic Signal 7 2 PMID: 19236702
Babola et al (2021) Purinergic signaling controls spontaneous activity in the auditory system throughout early development. J.Neurosci. 41 594 PMID: 33303678
Dosch et al (2019) Connexin-43-dependent ATP release mediates macrophage activation during sepsis. Elife 8 PMID: 30735126
Konopatskaya et al (2009) PKCalpha regulates platelet granule secretion and thrombus formation in mice. J Clin Invest 119 399 PMID: 19147982
Braganhol et al (2015) Nucleotide receptors control IL-8/CXCL8 and MCP-1/CCL2 secretions as well as proliferation in human glioma cells. Biochim Biophys Acta 1852 120 PMID: 25445541
Alefishat et al (2013) Antagonism of P2Y1-induced vasorelaxation by acyl CoA: a critical role for palmitate and 3'-phosphate. Br J Pharmacol 168 1911 PMID: 23215951
Fei et al (2013) Neurogenic mucosal bicarbonate secretion in guinea pig duodenum. Br J Pharmacol 168 880 PMID: 22994306
Helms et al (2013) Mechanisms of hemolysis-associated platelet activation. J Thromb Haemost 11 2148 PMID: 24119131
Ilatovskaya et al (2013) Pharmacological characterization of the P2 receptors profile in the podocytes of the freshly isolated rat glomeruli. Am J Physiol Cell Physiol 305 C1050 PMID: 24048730
Ohtani et al (2008) Evidence for the possible involvement of the P2Y(6) receptor in Ca (2+) mobilization and Ins secretion in mouse pancreatic islets. Purinergic Signal 4 365 PMID: 18784987
Ryu et al (2017) Paradoxical induction of growth arrest and apoptosis by EGF via the up-regulation of PTEN by activating Redox factor-1/Egr-1 in human lung cancer cells. Oncotarget 8 4181 PMID: 27935858
Bradley et al (2010) Novel excitatory effects of adenosine triphosphate on contractile and pacemaker activity in rabbit urethral smooth muscle. J Urol 183 801 PMID: 20022059
Duffy et al (2012) Changes in neuromuscular transmission in the W/W(v) mouse internal anal sphincter. Neurogastroenterol Motil 24 e41 PMID: 22074497
Gorman et al (2010) Adenine nucleotide control of coronary blood flow during exercise. Am J Physiol Heart Circ Physiol 299 H1981 PMID: 20852039
Baron et al (2015) The NLRP3 inflammasome is activated by nanoparticles through ATP, ADP and adenosine. Thromb J 6 e1629 PMID: 25654762
Ham et al (2010) Endogenous luminal surface adenosine signaling regulates duodenal bicarbonate secretion in rats. J Cell Biochem 335 607 PMID: 20805305
Liu et al (2018) Salvianolic acids from antithrombotic Traditional Chinese Medicine Danshen are antagonists of human P2Y1 and P2Y12 receptors. Sci Rep 8 11380 PMID: 30038283
Babola et al (2020) Purinergic signaling in cochlear supporting cells reduces hair cell excitability by increasing the extracellular space. Elife 9 e52160 PMID: 31913121
Erdélyi et al (2014) Analyzing receptor assemblies in the cell membrane using fluorescence anisotropy imaging with TIRF microscopy. PLoS One 9 e100526 PMID: 24945870
Kurahashi et al (2014) Platelet-derived growth factor receptor-α-positive cells and not smooth muscle cells mediate purinergic hyperpolarization in murine colonic muscles. Am J Physiol Cell Physiol 307 C561 PMID: 25055825
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