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Submit ReviewMRS 2279
Discontinued Product
This product has been withdrawn from sale and is superseded by MRS 2500 tetraammonium salt (Cat. No. 2159)
说明： Selective, high affinity P2Y1 antagonist
化学名： (1R*,2S*)-4-[2-Chloro-6-(methylamino)-9H-purin-9-yl]-2-(phosphonooxy)bicyclo[3.1.0]hexane-1-methanol dihydrogen phosphate ester diammonium salt
纯度： ≥98% (HPLC)
生物活性 for MRS 2279
MRS 2279 is a selective, high affinity competitive antagonist of the P2Y1 receptor (Ki = 2.5 nM; IC50 = 51.6 nM). Fails to block nucleotide signaling at most other P2Y receptors (P2Y2, P2Y4, P2Y6, P2Y11 and P2Y12) and potently inhibits ADP-induced aggregation of human blood platelets in vitro (pKB = 8.05).
许可信息
Sold under license from the NIH, US Patent 10/169975
技术数据 for MRS 2279
| 分子量 | 503.78 |
| 公式 | C13H18ClN5O8P2.2NH3 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2387505-47-5 |
| PubChem ID | 90488744 |
| InChI Key | MLPKPDFUVMQAOX-KOVKCLEESA-N |
| Smiles | ClC4=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 |
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.
产品说明书 for MRS 2279
参考文献 for MRS 2279
参考文献是支持产品生物活性的出版物。
Nandanan et al (2000) Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y1 receptor ligands. J.Med.Chem. 43 829 PMID: 10715151
Boyer et al (2002) 2-Chloro N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate is a selective high affinity P2Y1 receptor antagonist. Br.J.Pharmacol. 135 2004 PMID: 11959804
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
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关键词: MRS 2279, MRS 2279 supplier, Selective, high, affinity, P2Y1, antagonists, Receptors, Purinergic, purinoceptors, MRS2279, 264611-07-6, 367909-40-8, antagonises, inhibitors, inhibits, P2Y, 2158, Tocris Bioscience
5 篇 MRS 2279 的引用文献
引用文献是使用了 Tocris 产品的出版物。 MRS 2279 的部分引用包括：
Ohtomo et al (2011) Increase of intracellular Ca2+ by purinergic receptors in cultured rat lacrimal gland myoepithelial cells. Invest Ophthalmol Vis Sci 52 9503 PMID: 22039237
Wilkaniec et al (2017) P2X7 receptor-pannexin 1 interaction mediates extracellular alpha-synuclein-induced ATP release in neuroblastoma SH-SY5Y cells. Purinergic Signal 13 347 PMID: 28516276
Dosch et al (2019) Connexin-43-dependent ATP release mediates macrophage activation during sepsis. Elife 8 PMID: 30735126
Harper and Poole (2010) Protein kinase Ctheta negatively regulates store-independent Ca2+ entry and phosphatidylserine exposure downstream of glycoprotein VI in platelets. J Biol Chem 285 19865 PMID: 20388711
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. Cell Death Dis 31 1930 PMID: 21487414
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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.