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Submit ReviewMRS 2365
说明： Highly potent and selective P2Y1 agonist
化学名： [[(1R,2R,3S,4R,5S)-4-[6-Amino-2-(methylthio)-9H-purin-9-yl]-2,3-dihydroxybicyclo[3.1.0]hex-1-yl]methyl] diphosphoric acid mono ester trisodium salt
纯度： ≥98% (HPLC)
生物活性 for MRS 2365
MRS 2365 is a highly potent, selective P2Y1 receptor agonist (EC50 = 0.4 nM). Displays no activity at P2Y12 receptors and only very low agonist activity at P2Y13 receptors (at concentrations up to 1 μM). Increases the upregulation of NTPDase1 by ATPγS.
许可信息
Sold under license from the NIH, US Patent 10/169975
技术数据 for MRS 2365
| 分子量 | 549.28 |
| 公式 | C13H16N5O9P2SNa3 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| PubChem ID | 73755043 |
| InChI Key | ZYPJOXVKTCEBCA-PVMCGCOJSA-K |
| Smiles | [Na+].[Na+].[Na+].CSC1=NC(N)=C2N=CN(C3[C@H]4C[C@@]4(COP([O-])(=O)OP([O-])([O-])=O)[C@@H](O)[C@H]3O)C2=N1 |
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 2365
| 溶解性 | Soluble in water (supplied pre-dissolved at a concentration of 10mM) |
产品说明书 for MRS 2365
参考文献 for MRS 2365
参考文献是支持产品生物活性的出版物。
Ravi et al (2002) Adenine nucleotide analogues locked in a northern methanocarba conformation: enhanced stability and potency as P2Y1 receptor agonists. J.Med.Chem. 45 2090 PMID: 11985476
Chhatriwala et al (2004) Induction of novel agonist selectivity for the ADP-activated P2Y1 receptor versus the ADP-activated P2Y12 and P2Y13 receptors by conformational constraint of an ADP analog. J.Pharmacol.Exp.Ther. 311 1038 PMID: 15345752
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 2365, please let us know.
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关键词: MRS 2365, MRS 2365 supplier, potent, selective, P2Y1, agonists, Receptors, Purinergic, purinoceptors, MRS2365, 436847-09-5, P2Y, 2157, Tocris Bioscience
11 篇 MRS 2365 的引用文献
引用文献是使用了 Tocris 产品的出版物。 MRS 2365 的部分引用包括：
Shabir et al (2013) Functional expression of purinergic P2 receptors and transient receptor potential channels by the human urothelium. Neuropsychopharmacology 305 F396 PMID: 23720349
Gao et al (2013) The role of P2Y(14) and other P2Y receptors in degranulation of human LAD2 mast cells. J Cereb Blood Flow Metab 9 31 PMID: 22825617
Chandaka et al (2011) Facilitation of transmitter release from rat sympathetic neurons via presynaptic P2Y(1) receptors. Br J Pharmacol 164 1522 PMID: 21557728
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
Zhang et al (2019) P2Y1 Purinergic Receptor Modulate Axon Initial Segment Initial Development. Front Cell Neurosci 13 152 PMID: 31068791
Koch et al (2015) Impaired cognition after stimulation of P2Y1 receptors in the rat medial prefrontal cortex. J Cereb Blood Flow Metab 40 305 PMID: 25027332
Stefanini et al (2015) RASA3 is a critical inhibitor of RAP1-dependent platelet activation. J Neurosci 125 1419 PMID: 25705885
Filippov et al (2010) The scaffold protein NHERF2 determines the coupling of P2Y1 nucleotide and mGluR5 glutamate receptor to different ion channels in neurons. Pharmacol Res 30 11068 PMID: 20720114
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
Kuboyama et al (2011) Astrocytic P2Y(1) receptor is involved in the regulation of cytokine/chemokine transcription and cerebral damage in a rat model of cerebral ischemia. J Clin Invest 31 1930 PMID: 21487414
Mamedova et al (2008) Attenuation of apoptosis in vitro and ischemia/reperfusion injury in vivo in mouse skeletal muscle by P2Y6 receptor activation. Purinergic Signal 58 232 PMID: 18805489
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
P2X and P2Y Receptors Scientific Review
Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.