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Description: Blocker of VRAC/ICl, swell
Alternative Names: SN-401
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)
Biological Activity for DCPIB
DCPIB 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.
Technical Data for DCPIB
| 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 for DCPIB
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| ethanol | 42.74 | 100 |
Preparing Stock Solutions for DCPIB
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 for DCPIB
References for DCPIB
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
Lahey et al (2020) LRRC8A:C/E heteromeric channels are ubiquitous transporters of cGAMP. Mol.Cell. 80 1 PMID: 33171122
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Keywords: 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
17 Citations for DCPIB
Citations are publications that use Tocris products. Selected citations for DCPIB include:
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
Do you know of a great paper that uses DCPIB from Tocris? Please let us know.
Reviews for DCPIB
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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.