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Purity: ≥98%
DCPIB (an ethacrynic acid derivative) is a novel, potent and selective blocker of the volume-sensitive anion channel (VSAC) on electrical activity and insulin secretion in rat pancreatic beta-cells. DCPIB inhibited whole-cell VSAC currents in beta-cells with IC50 values of 2.2 and 1.7 microM for inhibition of outward and inward currents, respectively. DCPIB also inhibited the VSAC at the single channel level in cells activated by glucose. In intact cells, DCPIB caused a net increase in beta-cell input conductance and evoked an outward current that was sensitive to inhibition by tolbutamide, suggesting KATP channel activation. However, no KATP channel activation was evident under conventional whole-cell conditions, suggesting that the drug might activate the channel in intact cells via an indirect mechanism, possibly involving nutrient metabolism. DCPIB suppressed glucose-induced electrical activity in beta-cells, hyperpolarised the cell membrane potential at a substimulatory glucose concentration and prevented depolarisation when the glucose concentration was raised to stimulatory levels. The suppression of electrical activity by DCPIB was associated with a marked inhibition of glucose-stimulated insulin release from intact islets. It is concluded that DCPIB inhibits electrical and secretory activity in the beta-cell as a combined result of a reciprocal inhibition of VSAC and activation of KATP channel activities, thus producing a marked hyperpolarisation of the beta-cell membrane potential.
| ln Vitro |
In COS-7 cells, DCPIB (10 μM) increases TRAAK currents and activates TREK1 [1]. With an IC50 of 0.14 μM, DCPIB (10 μM) substantially and reversibly suppresses TRESK currents in COS-7 cells [1]. In CPAE cells, 10 μM had no discernible inhibitory effect on ICl, swell circulation, or ICl, Ca [2]. The effects of DCPIB (10 μM, 5 min) on cardiomyocyte vascular layer edema are insignificant [2]. In BV2 cells, LPS-induced MAPK activation is inhibited by DCPIB (10 μM, 3 h) [3].
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| ln Vivo |
Improved neuronal injury and inhibition of astrocyte activation by rMCAO deposition are two benefits of LDN-212854 (intracerebroventricular infusion, 1 mM, 10 μL) [3].
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| Cell Assay |
Immunofluorescence [3]
Cell Types: BV2 Cell Tested Concentrations: 10 μM Incubation Duration: 3 h Experimental Results: Ki67-positive staining of microglia and pro was Dramatically diminished. -Secretion of inflammatory cytokines (TNF-α, IL-1β). Western Blot Analysis[3] Cell Types: BV2 Cells Tested Concentrations: 10 μM Incubation Duration: 3 hrs (hours) Experimental Results: The migration potential of BV2 cells exposed to brief OGD (hypoxia-glucose deprivation) was inhibited. |
| Animal Protocol |
Animal/Disease Models: Reversible middle cerebral artery occlusion (rMCAO) model [3]: 1 mM, 10 μL
Route of Administration: Manual administration via intracerebroventricular infusion for 20 seconds Experimental Results: Pyramidal neuronal damage caused by rMCAO in the CA1 region was diminished. |
| References |
[1]. Lv J, et al. DCPIB, an Inhibitor of Volume-Regulated Anion Channels, Distinctly Modulates K2P Channels. ACS Chem Neurosci. 2019 Apr 17.
[2]. Decher N, et al. DCPIB is a novel selective blocker of I(Cl,swell) and prevents swelling-induced shortening of guinea-pig atrial action potential duration. Br J Pharmacol. 2001 Dec;134(7):1467-79. [3]. Qingdong Han, et al. DCPIB, a potent volume-regulated anion channel antagonist, attenuates microglia-mediated inflammatory response and neuronal injury following focal cerebral ischemia. Brain Res. 2014 Jan 13;1542:176-85. |
| Molecular Formula |
82749-70-0
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| Molecular Weight |
427.37
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| CAS # |
82749-70-0
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| SMILES |
CCCCC1(CC2=C(C1=O)C(Cl)=C(Cl)C(OCCCC(O)=O)=C2)C1CCCC1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3399 mL | 11.6995 mL | 23.3989 mL | |
| 5 mM | 0.4680 mL | 2.3399 mL | 4.6798 mL | |
| 10 mM | 0.2340 mL | 1.1699 mL | 2.3399 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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