PSB 0739

Name: PSB 0739
Brand: Tocris Bioscience
SKU: 3983
Rating: 4 (2 reviews)

Cat. No. 3983 15 篇引用文献 2 条评论提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Highly potent P2Y₁₂ antagonist

化学名： 1-Amino-9,10-dihydro-9,10-dioxo-4-[[4-(phenylamino)-3-sulfophenyl]amino]-2-anthracenesulfonic acid sodium salt

纯度： ≥95% (HPLC)

说明书

引用文献 (15)

文献 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for PSB 0739

PSB 0739 is a highly potent P2Y₁₂ receptor antagonist (K_i = 24.9 nM). Unlike clopidogrel (Cat. No. 2490), does not require bioactivation.

许可信息

Sold with the permission of the University of Bonn.

技术数据 for PSB 0739

分子量	609.54
公式	C₂₆H₁₇N₃Na₂O₈S₂
储存	Desiccate at RT
纯度	≥95% (HPLC)
CAS Number	1052087-90-7
PubChem ID	44583582
InChI Key	QBLLYXXXOJUNCV-UHFFFAOYSA-L
Smiles	[Na+].[Na+].NC1=C(C=C(NC2=CC(=C(NC3=CC=CC=C3)C=C2)S([O-])(=O)=O)C2=C1C(=O)C1=CC=CC=C1C2=O)S([O-])(=O)=O

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 PSB 0739

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	water	15.24	25

制备储备液 for PSB 0739

以下数据基于产品分子量 609.54。 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
0.25 mM	6.56 mL	32.81 mL	65.62 mL
1.25 mM	1.31 mL	6.56 mL	13.12 mL
2.5 mM	0.66 mL	3.28 mL	6.56 mL
12.5 mM	0.13 mL	0.66 mL	1.31 mL

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产品说明书 for PSB 0739

分析证书/产品说明书

化学品安全技术说明书

参考文献 for PSB 0739

参考文献是支持产品生物活性的出版物。

Hoffmann et al (2009) Interaction of new, very potent non-nucleotide antagonists with Arg256 of the human platelet P2Y₁₂ receptor. J.Pharmacol.Exp.Ther. 331 648 PMID: 19690189

Baqi et al (2009) High-affinity, non-nucleotide-derived competitive antagonists of platelet P2Y₁₂ receptors. J.Med.Chem. 52 3784 PMID: 19463000

Felix et al (2011) Development of a comprehensive set of P2 receptor pharmacological research compounds. Purinerg.Sig. 8 101 PMID: 22052555

If you know of a relevant reference for PSB 0739, please let us know.

按标靶查看相关产品

Purinergic (P2Y) Receptors

关键词: PSB 0739, PSB 0739 supplier, PSB0739, potent, selective, p2y12, purine, receptors, antagonists, purinoceptors, purinergic, antagonises, inhibitors, inhibits, Purinergic, P2Y, Receptors, 3983, Tocris Bioscience

15 篇 PSB 0739 的引用文献

引用文献是使用了 Tocris 产品的出版物。 PSB 0739 的部分引用包括：

Mária et al (2021) Involvement of P2Y12 receptors in a nitroglycerin-induced model of migraine in male mice. Br J Pharmacol 178 4626-4645 PMID: 34363208

Nishimura et al (2015) The Suramin Derivative NF449 Interacts with the 5-fold Vertex of the Enterovirus A71 Capsid to Prevent Virus Attachment to PSGL-1 and Heparan Sulfate. PLoS Pathog 11 e1005184 PMID: 26430888

Wang et al (2014) Nucleolin down-regulation is involved in ADP-induced cell cycle arrest in S phase and cell apoptosis in vascular endothelial cells. PLoS One 9 e110101 PMID: 25290311

Uderhardt et al (2019) Resident Macrophages Cloak Tissue Microlesions to Prevent Neutrophil-Driven Inflammatory Damage. Cell 177 541 PMID: 30955887

Smith et al (2017) Protease-activated receptor-4 and P2Y12 Dimerize, Co-Internalize and Activate Akt Signaling via Endosomal Recruitment of β-arrestin. J Biol Chem PMID: 28652403

Aungraheeta et al (2016) Inverse agonism at the P2Y12 receptor and ENT1 transporter blockade contribute to platelet inhibition by ticagrelor. Blood 128 2717 PMID: 27694321

Domokos et al (2022) Microglia modulate blood flow, neurovascular coupling, and hypoperfusion via purinergic actions. J Exp Med 219 PMID: 35201268

Tibor et al (2022) The dualistic role of the purinergic P2Y12-receptor in an in vivo model of Parkinson's disease: Signalling pathway and novel therapeutic targets. Pharmacol Res 176 106045 PMID: 34968684

Stefano L et al (2022) TREM2 regulates purinergic receptor-mediated calcium signaling and motility in human iPSC-derived microglia. Elife 11 PMID: 35191835

Takayama et al (2016) Diurnal dynamic behavior of microglia in response to infected bacteria through the UDP-P2Y6 receptor system Scientific Reports 6 30006 PMID: 27445174

Alice et al (2020) Antiplatelet Drug Ticagrelor Enhances Chemotherapeutic Efficacy by Targeting the Novel P2Y12-AKT Pathway in Pancreatic Cancer Cells. Cancers (Basel) 12 PMID: 31968611

Anne-Mette et al (2020) Prevention of P2 Receptor-Dependent Thrombocyte Activation by Pore-Forming Bacterial Toxins Improves Outcome in A Murine Model of Urosepsis. Int J Mol Sci 21 PMID: 32781764

Abud et al (2017) iPSC-Derived Human Microglia-like Cells to Study Neurological Diseases. Neuron 94 278 PMID: 28426964

Cserép et al (2020) Microglia Monitor and Protect Neuronal Function Through Specialized Somatic Purinergic Junctions. Science 367 528 PMID: 31831638

Madry et al (2018) Microglial Ramification, Surveillance, and Interleukin-1β Release Are Regulated by the Two-Pore Domain K+ Channel THIK-1. Neuron 97 299 PMID: 29290552

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PSB 0739 的评论

平均评分: 4 (基于 2 条评论。)

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Good inhibitor.

By Anonymous on 06/06/2020

分析类型： In Vivo

种属： Mouse

细胞系/组织： phagocyte

H20; dilution 10 μM

P2Y12 blocker.

By Anonymous on 01/30/2018

分析类型： Ex Vivo

种属： Mouse

细胞系/组织： acute brain slice

Used to block P2Y12 in acute brain slices. Monitored was the motility of microglia. No significant effect was found.

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.