DCPIB

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Cat.No. 1540 - DCPIB | C22H28Cl2O4 | CAS No. 82749-70-0
Description: Blocker of VRAC/ICl, swell
Chemical Name: 4-[(2-Butyl-6,7-dichloro-2-cyclopentyl-2,3-dihydro-1-oxo-1H-inden-5-yl)oxy]butanoic acid
Purity: ≥98% (HPLC)
Datasheet
Citations (15)
Reviews (1)
Literature (1)

Biological Activity

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.

Technical Data

M. Wt 427.37
Formula C22H28Cl2O4
Storage Store at +4°C
Purity ≥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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 42.74 100

Preparing Stock Solutions

The following data is based on the product molecular weight 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.

Concentration / Solvent Volume / Mass 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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

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


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

View Related Products by Product Action

View all Other Chloride Channel Blockers

Keywords: DCPIB, DCPIB supplier, Selective, blockers, VSAC, VRAC, IClswell, volume-sensitive, anion, channels, chloride, volume, regulated, Other, Chloride, Channels, Two-P, Potassium, 1540, Tocris Bioscience

15 Citations for DCPIB

Citations are publications that use Tocris products. Selected citations for DCPIB include:

Wong et al (2018) Swelling-induced chloride current in glioblastoma proliferation, migration, and invasion. J Cell Physiol 233 363 PMID: 28262948

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

Schlichter et al (2010) Swelling activated Cl- channels in microglia: Biophysics, pharmacology and role in glutamate release. Channels (Austin) 5 128 PMID: 21150294

Raucci et al (2010) Exogenous and endogenous ceramides elicit volume-sensitive chloride current in ventricular myocytes. Cardiovasc Res 86 55 PMID: 20008476

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

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

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

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

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

Hawkins et al (2013) Electrophysiological characteristics of enteric neurons isolated from the immortomouse. Proc Natl Acad Sci U S A 58 1516 PMID: 23371009

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

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

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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Reviews for DCPIB

Average Rating: 4 (Based on 1 Review.)

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a VRACs blocker.
By Anonymous on 02/02/2018
Assay Type: Ex Vivo
Species: Rat

DCPIB is a volume regulated anion channel. We used at 20-30microM in rat brain slice.


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