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Submit ReviewDCPIB is a volume-regulated anion channel (VRAC) blocker (IC50 ~ 2 μM in rat pancreatic β-cells). Also blocks ICl,swell in various cardiovascular tissues (IC50 = 4.1 μM in CPAE cells). Inhibits glucose-stimulated insulin secretion in intact β-cells via VSAC inhibition and indirect KATP channel activation. Reverses cell swelling-induced action potential duration shortening in atrial myocytes and inhibits astroglial swelling in vitro. Also activates TREK1 and TRAAK K+ channels and inhibits TRESK, TASK1 and TASK3 K+ channels at 10 μM, in vitro. Also inhibits VRAC-mediated 2'3'-cyclic-GMP-AMP (cGAMP) transport.
分子量 | 427.37 |
公式 | C22H28Cl2O4 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 82749-70-0 |
PubChem ID | 10071166 |
InChI Key | KHKGTPJPBOQECW-UHFFFAOYSA-N |
Smiles | CCCCC1(CC2=C(C1=O)C(Cl)=C(Cl)C(OCCCC(O)=O)=C2)C1CCCC1 |
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 | |||
ethanol | 42.74 | 100 |
以下数据基于产品分子量 427.37。 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 | 2.34 mL | 11.7 mL | 23.4 mL |
5 mM | 0.47 mL | 2.34 mL | 4.68 mL |
10 mM | 0.23 mL | 1.17 mL | 2.34 mL |
50 mM | 0.05 mL | 0.23 mL | 0.47 mL |
参考文献是支持产品生物活性的出版物。
Bourke et al (1981) Adenosine-stimulated astroglial swelling in cat cerebral cortex in vivo with total inhibition by a non-diuretic acylaryloxyacid derivative. J.Neurosurg. 55 364 PMID: 6267227
Decher et al (2001) DCPIB is a novel selective blocker of ICl,swell and prevents swelling-induced shortening of guinea-pig atrial action potential duration. Br.J.Pharmacol. 134 1467 PMID: 11724753
Best et al (2004) Inhibition of glucose-induced electrical activity in rat pancreatic β-cells by DCPIB, a selective inhibitor of volume-sensitive anion currents. Eur.J.Pharmacol. 489 13 PMID: 15063150
Lv et al (2019) DCPIB, an inhibitor of volume-regulated anion channels, distinctly modulates K2P channels. ACS.Chem.Neurosci. 10 2786 PMID: 30935201
Lahey et al (2020) LRRC8A:C/E heteromeric channels are ubiquitous transporters of cGAMP. Mol.Cell. 80 1 PMID: 33171122
If you know of a relevant reference for DCPIB, please let us know.
关键词: DCPIB, DCPIB supplier, Selective, blockers, VSAC, VRAC, IClswell, volume-sensitive, anion, channels, chloride, volume, regulated, LRRC8, cGAMP, transporter, transports, inhibits, inhibitor, inhibitors, K2P, SN401, SN-401, Other, Chloride, Channels, Two-P, Potassium, STING-Dependent, Signaling, 1540, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 DCPIB 的部分引用包括:
Hyzinski-García et al (2011) Hypo-osmotic swelling modifies glutamate-glutamine cycle in the cerebral cortex and in astrocyte cultures. J Neurochem 118 140 PMID: 21517854
Wong et al (2018) Swelling-induced chloride current in glioblastoma proliferation, migration, and invasion. J Cell Physiol 233 363 PMID: 28262948
Lahey et al (2020) LRRC8A:C/E heteromeric channels are ubiquitous transporters of cGAMP. Mol Cell 80 1 PMID: 33171122
Woo et al (2019) Pharmacological Dissection of Intrinsic Optical Signal Reveals a Functional Coupling between Synaptic Activity and Astrocytic Volume Transient. Exp Neurobiol 28 30 PMID: 30853822
Li et al (2012) Mechanisms of ATP release by human trabecular meshwork cells, the enabling step in purinergic regulation of aqueous humor outflow. J Cell Physiol 227 172 PMID: 21381023
Raucci et al (2010) Exogenous and endogenous ceramides elicit volume-sensitive chloride current in ventricular myocytes. Cardiovasc Res 86 55 PMID: 20008476
Takada et al (2014) Mechanosensitive ATP release from hemichannels and Ca2+ influx through TRPC6 accelerate wound closure in keratinocytes. Dig Dis Sci 127 4159 PMID: 25097230
Schlichter et al (2010) Swelling activated Cl- channels in microglia: Biophysics, pharmacology and role in glutamate release. Channels (Austin) 5 128 PMID: 21150294
Han et al (2019) Tweety-homolog (Ttyh) Family Encodes the Pore-forming Subunits of the Swelling-dependent Volume-regulated Anion Channel (VRACswell) in the Brain. Exp Neurobiol 28 183 PMID: 31138989
Zhang et al (2008) DCPIB, a specific inhibitor of volume regulated anion channels (VRACs), reduces infarct size in MCAo and the release of glutamate in the ischemic cortical penumbra. Exp Neurol 210 514 PMID: 18206872
Draganov et al (2015) Modulation of P2X4/P2X7/Pannexin-1 sensitivity to extracellular ATP via iverm. induces a non-apoptotic and inflammatory form of cancer cell death. J Cell Sci 5 16222 PMID: 26552848
Catalán et al (2015) A fluid secretion pathway unmasked by acinar-specific Tmem16A gene ablation in the adult mouse salivary gland. Int J Clin Exp Med 112 2263 PMID: 25646474
Gunasekar et al (2022) Small molecule SWELL1 complex induction improves glycemic control and nonalcoholic fatty liver disease in murine Type 2 diabetes. Nat.Commun. 13 784 PMID: 35145074
Ghosh et al (2017) Leucine-rich repeat-containing 8B protein is associated with the endoplasmic reticulum Ca2+ leak in HEK293 cells. J Cell Sci 130 3818 PMID: 28972132
Li and Olson (2008) Purinergic activation of anion conductance and osmolyte efflux in cultured rat hippocampal neurons. Am J Physiol Cell Physiol 295 C1550 PMID: 18923056
Hawkins et al (2013) Electrophysiological characteristics of enteric neurons isolated from the immortomouse. Proc Natl Acad Sci U S A 58 1516 PMID: 23371009
Sabirov et al (2013) Volume-sensitive anion channels mediate osmosensitive glutathione release from rat thymocytes. PLoS One 8 e55646 PMID: 23383255
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DCPIB is a volume regulated anion channel. We used at 20-30microM in rat brain slice.