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Submit Review5-BDBD is a potent and selective P2X4 receptor antagonist. Blocks P2X4-mediated currents in Chinese hamster ovary cells (IC50 = 0.50 μM). Exhibits no significant antagonist effects at other P2X receptors. Reduces long-term potentiation (LTP) in rat hippocampal slices.
分子量 | 355.19 |
公式 | C17H11BrN2O2 |
储存 | Store at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 768404-03-1 |
PubChem ID | 9841560 |
InChI Key | NKYMVQPXXTZHSF-UHFFFAOYSA-N |
Smiles | BrC1=CC(C(C3=C4C2=C(O3)C=CC=C2)=NCC(N4)=O)=CC=C1 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 35.52 | 100 |
以下数据基于产品分子量 355.19。 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 |
---|---|---|---|
1 mM | 2.82 mL | 14.08 mL | 28.15 mL |
5 mM | 0.56 mL | 2.82 mL | 5.63 mL |
10 mM | 0.28 mL | 1.41 mL | 2.82 mL |
50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
参考文献是支持产品生物活性的出版物。
Donnelly-Roberts et al (2008) Painful purinergic receptors. J.Pharmacol.Exp.Ther. 324 409 PMID: 18042830
Casati et al (2011) Cell-autonomous regulation of hematopoietic stem cell cycling activity by ATP. Cell Death Differ. 18 396 PMID: 20798687
Coddou et al (2018) Characterization of the antagonist actions of 5-BDBD at the rat P2X4 receptor. Neurosci Lett. 690 219 PMID: 30366010
If you know of a relevant reference for 5-BDBD, please let us know.
关键词: 5-BDBD, 5-BDBD supplier, potent, P2X4, antagonists, purinergic, receptors, BDBD, selective, P2X, Receptors, 3579, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 5-BDBD 的部分引用包括:
Mascanfroni et al (2015) Metabolic control of type 1 regulatory T cell differentiation by AHR and HIF1-α. Circulation 21 638 PMID: 26005855
Miguel Cruz & Beall (2020) Extracellular ATP Increases Glucose Metabolism in Skeletal Muscle Cells in a P2 Receptor Dependent Manner but Does Not Contribute to Palmitate-Induced Insulin Resistance. Front Physiol 11 PMID: 33101053
Dhuna et al (2019) Ginsenosides Act As Positive Modulators of P2X4 Receptors. Mol Pharmacol 95 210 PMID: 30545933
Kawano et al (2015) Autocrine Regulation of UVA-Induced IL-6 Production via Release of ATP and Activation of P2Y Receptors. PLoS One 10 e0127919 PMID: 26030257
Shabir et al (2013) Functional expression of purinergic P2 receptors and transient receptor potential channels by the human urothelium. Nat Med 305 F396 PMID: 23720349
Vergani et al (2013) Long-term heart transplant survival by targeting the ionotropic purinergic receptor P2X7. J Biol Chem 127 463 PMID: 23250993
Wu et al (2011) Functional expression of P2X4 receptor in capillary endothelial cells of the cochlear spiral ligament and its role in regulating the capillary diameter. Am J Physiol Heart Circ Physiol 301 H69 PMID: 21460192
Dosch et al (2019) Connexin-43-dependent ATP release mediates macrophage activation during sepsis. Elife 8 PMID: 30735126
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
Vladislav et al (2021) Characterization of purinergic receptor 2 signaling in podocytes from diabetic kidneys. iScience 24 102528 PMID: 34142040
Timothy S et al (2021) Differential Regulation of ATP- and UTP-Evoked Prostaglandin E2 and IL-6 Production from Human Airway Epithelial Cells. J Immunol 207 1275-1287 PMID: 34389624
Rui et al (2021) Astragalin Alleviates Neuropathic Pain by Suppressing P2X4-Mediated Signaling in the Dorsal Root Ganglia of Rats. Front Neurosci 14 570831 PMID: 33505232
Aron M et al (2018) Keratinocytes mediate innocuous and noxious touch via ATP-P2X4 signaling. Elife 7 PMID: 29336303
Trabanelli et al (2012) Extracellular ATP exerts opposite effects on activated and regulatory CD4+ T cells via purinergic P2 receptor activation. J Immunol 189 1303 PMID: 22753942
Nörenberg et al (2012) Positive allosteric modulation by iverm. of human but not murine P2X7 receptors. Br J Pharmacol 167 48 PMID: 22506590
László et al (2022) Motoneuronal inflammasome activation triggers excessive neuroinflammation and impedes regeneration after sciatic nerve injury. J Neuroinflammation 19 68 PMID: 35305649
Vladislav et al (2022) Modulation of P2X4 receptor activity by ivermectin and 5-BDBD has no effect on the development of ARPKD in PCK rats. Physiol Rep 10 e15510 PMID: 36353932
Zumerle et al (2019) Intercellular Calcium Signaling Induced by ATP Potentiates Macrophage Phagocytosis. Cell Rep 27 1 PMID: 30943393
Uderhardt et al (2019) Resident Macrophages Cloak Tissue Microlesions to Prevent Neutrophil-Driven Inflammatory Damage. Cell 177 541 PMID: 30955887
Raghava et al (2014) P2X4 receptor regulates alcohol-induced responses in microglia. J Neuroimmune Pharmacol 9 668-78 PMID: 25135400
Belinda L et al (2020) Pharmacological and genetic characterisation of the canine P2X4 receptor. Br J Pharmacol 177 2812-2829 PMID: 32017039
Ledderose et al (2016) Mitochondrial Dysfunction, Depleted Purinergic Signaling, and Defective T Cell Vigilance and Immune Defense. J Infect Dis 213 456 PMID: 26150546
Gofman et al (2016) Relative Role of Akt, ERK and CREB in Alcohol-Induced Microglia P2X4R Receptor Expression. Alcohol Alcohol 51 647 PMID: 26946194
Peng et al (2016) Purinergic and store-operated Ca(2+) signaling mechanisms in mesenchymal stem cells and their roles in ATP-induced stimulation of cell migration. Stem Cells 34 2102 PMID: 27038239
Chen et al (2016) Effect of P2X4R on airway inflammation and airway remodeling in allergic airway challenge in mice. Mol Med Rep 13 697 PMID: 26648454
Maslieieva and Thompson (2014) A critical role for pannexin-1 in activation of innate immune cells of the choroid plexus. Channels (Austin) 8 131 PMID: 24418937
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平均评分: 5 (Based on 1 Review.)
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