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Submit Review2-APB
说明： IP3 receptor antagonist. Also TRP channel modulator
化学名： 2-Aminoethoxydiphenylborane
纯度： ≥98% (HPLC)
生物活性 for 2-APB
2-APB is a functional and membrane permeable D-myo-inositol 1,4,5-trisphosphate (IP3) receptor antagonist (IC50 = 42 μM). Stimulates store-operated calcium (SOC) release at low concentrations (< 10 μM) and inhibits it at higher concentrations (up to 50 μM). Increases STIM-Orai channel conductance and limits ion selectivity. Modulator of TRP channels; blocks TRPC1, TRPC3, TRPC5, TRPC6, TRPV6, TRPM3, TRPM7, TRPM8 and TRPP2 and at higher concentrations stimulates TRPV1, TRPV2 and TRPV3. Also blocks specific gap channel subtypes.
技术数据 for 2-APB
| 分子量 | 225.1 |
| 公式 | C14H16BNO |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 524-95-8 |
| PubChem ID | 1598 |
| InChI Key | BLZVCIGGICSWIG-UHFFFAOYSA-N |
| Smiles | NCCOB(C1=CC=CC=C1)C1=CC=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.
溶解性数据 for 2-APB
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 22.51 | 100 温和加热 |
制备储备液 for 2-APB
以下数据基于产品分子量 225.1。 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 | 4.44 mL | 22.21 mL | 44.42 mL |
| 5 mM | 0.89 mL | 4.44 mL | 8.88 mL |
| 10 mM | 0.44 mL | 2.22 mL | 4.44 mL |
| 50 mM | 0.09 mL | 0.44 mL | 0.89 mL |
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产品说明书 for 2-APB
参考文献 for 2-APB
参考文献是支持产品生物活性的出版物。
Bai et al (2006) Block of specific gap junction channel subtypes by 2-aminoethoxydiphenyl borate (2-APB). J.Pharmacol.Exp.Ther. 319 1452 PMID: 16985167
Maruyama et al (1997) 2APB, 2-aminoethoxydiphenyl borate, a membrane-penetrable modulator of Ins(1,4,5)P3-induced Ca2+ release. J.Biochem. 122 498 PMID: 9348075
Togashi et al (2008) Inhibition of the transient receptor potential cation channel TRPM2 by 2-aminoethoxydiphenyl borate (2-APB). Br.J.Pharmacol. 153 1324 PMID: 18204483
Varnai et al (2009) STIM and Orai: the long-awaited constituents of store-operated calcium entry. TiPs 30 118 PMID: 19187978
Xu et al (2005) Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltafe-dependent effect. Br.J.Pharmacol. 145 405 PMID: 15806115
If you know of a relevant reference for 2-APB, please let us know.
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关键词: 2-APB, 2-APB supplier, Increases, STIM-Orai, channels, conductivity, reduces, selectivity, IP3, receptor, antagonist, TRP, modulators, Store, Operated, Calcium, Channels, Ca2+, Inositol, 145-triphosphate, Receptors, Triphosphoinositol, Transient, Receptor, Potential, PIP2, Lipids, cAMP, Signaling, Signal, Non-selective, 1224, Tocris Bioscience
44 篇 2-APB 的引用文献
引用文献是使用了 Tocris 产品的出版物。 2-APB 的部分引用包括：
Nakakura et al (2015) Pathophysiological significance of the two-pore domain K(+) channel K2P5.1 in splenic CD4(+)CD25(-) T cell subset from a chemically-induced murine inflammatory bowel disease model. Cell Death Dis 6 299 PMID: 26578971
Baron et al (2015) The NLRP3 inflammasome is activated by nanoparticles through ATP, ADP and adenosine. Dev Neurobiol 6 e1629 PMID: 25654762
Flynn et al (2015) Activation of the neurokinin 3 receptor promotes filopodia growth and sprouting in rat embryonic hypothalamic cells. Carcinogenesis 75 44896 PMID: 25044785
Fransen et al (2015) Dissecting out the complex Ca2+-mediated phenylephrine-induced contractions of mouse aortic segments. PLoS One 10 e0121634 PMID: 25803863
Dobson et al (2015) Caffeine Modulates Vesicle Release and Recovery at Cerebellar Parallel Fibre Terminals, Independently of Calcium and Cyclic AMP Signalling. Biomed Res Int 10 e0125974 PMID: 25933382
Hutchins and Wray (2014) Capture of microtubule plus-ends at the actin cortex promotes axophilic neuronal migration by enhancing microtubule tension in the leading process. J Biol Chem 8 400 PMID: 25505874
Gonçalves et al (2014) Activation of a TRP-like channel and intracellular Ca2+ dynamics during phospholipase-C-mediated cell death. J Cell Sci 127 3817 PMID: 25037570
Hendron et al (2014) Potent functional uncoupling between STIM1 and Orai1 by dimeric 2-aminodiphenyl borinate analogs. Cell Calcium 56 482 PMID: 25459299
Kim et al (2010) Non-cardiomyocytes influence the electrophysiological maturation of human embryonic stem cell-derived cardiomyocytes during differentiation. Front Physiol 19 783 PMID: 20001453
Choi et al (2010) Caffeine and 2-Aminoethoxydiphenyl Borate (2-APB) Have Different Ability to Inhibit Intracellular Calcium Mobilization in Pancreatic Acinar Cell. J Neuroimmune Pharmacol 14 105 PMID: 20473382
Lim et al (2018) Neuronal Activity-Dependent Activation of Astroglial Calcineurin in Mouse Primary Hippocampal Cultures. Int J Mol Sci 19 PMID: 30274399
Huang et al (2012) SKF83959, an agonist of phosphatidylinositol-linked D(1)-like receptors, promotes ERK1/2 activation and cell migration in cultured rat astrocytes. Korean J Physiol Pharmacol 7 e49954 PMID: 23185493
Chow et al (2011) Calcium-sensing receptor modulates extracellular Ca(2+) entry via TRPC-encoded receptor-operated channels in human aortic smooth muscle cells. PLoS One 301 C461 PMID: 21562303
Tang et al (2015) Stimulation-evoked Ca2+ signals in astrocytic processes at hippocampal CA3-CA1 synapses of adult mice are modulated by glutamate and ATP. J Neurosci 35 3016 PMID: 25698739
Grimes et al (2014) Cross-synaptic synchrony and transmission of signal and noise across the mouse retina. Elife 3 e03892 PMID: 25180102
Tamura et al (2014) Both neurons and astrocytes exhibited tetrodotoxin-resistant metabotropic glutamate receptor-dependent spontaneous slow Ca2+ oscillations in striatum. PLoS One 9 e85351 PMID: 24454845
Hutchins et al (2013) Calcium release-dependent actin flow in the leading process mediates axophilic migration. J Pharmacol Exp Ther 33 11361 PMID: 23843509
Li et al (2013) Antagonism of neuronal prostaglandin E(2) receptor subtype 1 mitigates amyloid β neurotoxicity in vitro. Biochem Pharmacol 8 87 PMID: 22718277
Balasubramanian et al (2013) AMP-activated protein kinase as regulator of P2Y(6) receptor-induced Ins secretion in mouse pancreatic β-cells. Hypertension 85 991 PMID: 23333427
Chang et al (2013) Areca nut-induced buccal mucosa fibroblast contraction and its signaling: a potential role in oral submucous fibrosis--a precancer condition. Front Cell Neurosci 34 1096 PMID: 23349021
Aihara et al (2013) In vivo epithelial wound repair requires mobilization of endogenous intracellular and extracellular calcium. PLoS One 288 33585 PMID: 24121509
O'Malley et al (2020) TRPM4 Conductances in Thalamic Reticular Nucleus Neurons Generate Persistent Firing during Slow Oscillations J Neurosci 40 4813 PMID: 32414784
Florea et al (2017) Calcium-regulatory proteins as modulators of chemotherapy in human neuroblastoma. Oncotarget 8 22876 PMID: 28206967
Khrimian et al (2017) Gpr158 mediates osteocalcin's regulation of cognition. J Exp Med 214 2859 PMID: 28851741
Snetkov et al (2008) Low concentrations of sphingosylphosphorylcholine enhance pulmonary artery vasoreactivity: the role of protein kinase C δ and Ca2+ entry. Am J Physiol Cell Physiol 51 239 PMID: 18158336
Varadarajan et al (2013) Endoplasmic reticulum membrane reorganization is regulated by ionic homeostasis. PLoS One 8 e56603 PMID: 23457590
Lee et al (2011) Regulation of Substantia Nigra Pars Reticulata GABAergic Neuron Activity by H?O? via Flufenamic Acid-Sensitive Channels and K(ATP) Channels. Front Syst Neurosci 5 14 PMID: 21503158
Dong et al (2009) P2Y receptors mediate Ca2+ signaling in duodenocytes and contribute to duodenal mucosal bicarbonate secretion. Am J Physiol Gastrointest Liver Physiol 296 G424 PMID: 19074643
Sribnick et al (2009) Estrogen attenuates glutamate-induced cell death by inhibiting Ca2+ influx through L-type voltage-gated Ca2+ channels. Brain Res 1276 159 PMID: 19389388
Clark et al (2009) Adenosine-evoked hyperpolarization of retinal ganglion cells is mediated by G-protein-coupled inwardly rectifying K+ and small conductance Ca2+-activated K+ channel activation. J Neurosci 29 11237 PMID: 19741130
Zhao et al (2019) Cell sensing and decision-making in confinement: The role of TRPM7 in a tug of war between hydraulic pressure and cross-sectional area. Sci Adv 5 eaaw7243 PMID: 31355337
Kim et al (2019) Role of miRNA-181a-2-3p in cadmium-induced inflammatory responses of human bronchial epithelial cells. J Thorac Dis 11 3055 PMID: 31463135
Bagayogo and Dreyfus (2009) Regulated release of BDNF by cortical oligodendrocytes is mediated through metabotropic glutamate receptors and the PLC pathway. ASN Neuro 1 PMID: 19570026
Colavita et al (2016) Layer-specific potentiation of network GABAergic inhibition in the CA1 area of the hippocampus. Sci Rep 6 28454 PMID: 27345695
Chen et al (2010) The amiloride-sensitive epithelial Na+ channel PPK28 is essential for drosophila gustatory water reception. J Neurosci 30 6247 PMID: 20445050
Patel et al (2009) Mobilization of calcium from intracellular stores facilitates somatodendritic DA release. J Neurosci 29 6568 PMID: 19458227
Qin et al (2016) Connexin 32-mediated cell-cell communication is essential for hepatic differentiation from humanembryonic stem cells Scientific Reports 6 37388 PMID: 27874032
Begum et al (2012) DHA inhibits ER Ca2+ release and ER stress in astrocytes following in vitro ischemia. J Neurochem 120 622 PMID: 22129278
Lee et al (2012) The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP. Nature 492 123 PMID: 23143333
Facchinetti et al (2006) Nimodipine selectively stimulates beta-amyloid 1-42 secretion by a mechanism independent of calcium influx blockage. Neurobiol Aging 27 218 PMID: 16399208
Yamboliev (2005) PI3K and PKC contribute to membrane depolarization mediated by alpha2-adrenoceptors in the canine isolated mesenteric vein. BMC Physiol 5 9 PMID: 15958164
Gu et al (2005) 2-aminoethoxydiphenyl borate stimulates pulmonary C neurons via the activation of TRPV channels. Am J Physiol Lung Cell Mol Physiol 288 L932 PMID: 15653710
Kelm et al (2007) Calcium release from presynaptic internal stores is required for ethanol to increase spontaneous γ-aminobutyric acid release onto cerebellum Purkinje neurons. Stem Cells Dev 323 356 PMID: 17652632
Villalba et al (2007) Contribution of both Ca2+ entry and Ca2+ sensitization to the alpha1-adrenergic vasoconstriction of rat penile small arteries. Am J Physiol Heart Circ Physiol 292 H1157 PMID: 17085536
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Significantly inhibits TRPM7 current.
By
Yuyang Sun on 06/29/2022
分析类型： In Vitro
种属： Human
细胞系/组织： sh-sy5y
It significantly inhibits TRPM7 current. Very good.
2-APB reduces store-operated Ca2+ entry in HEK293 cells.
By
Anonymous on 07/10/2019
分析类型： In Vitro
种属： Human
细胞系/组织： HEK293
HEK293 cells were incubated with intracellular Ca2+ sensitive dye, Fura-2AM in normal tyrode solution for 40 min, washed and kept aside for 20 min. Fura2-loaded cells were excited alternately at 340 and 380 nm and fluorescence at 510 nm was expressed as 340/380 ratio. Intracellular Ca2+ stores were depleted with 30 μM BHQ which promotes store-operated Ca2+ entry into the cells upon addition of 1 mM extracellular Ca2+. Preincubation of cells with 50 μM 2-APB for 10 min reduces this Ca2+ entry.
2-APB in brains slices.
By
Anonymous on 03/08/2018
分析类型： Ex Vivo
种属： Mouse
2-APB (50uM) was applied to mouse brain slices while measuring evoked dopamine release.
Put it into DMSO (100mM).
