DCPIB
DCPIB is a volume-regulated anion channel (VRAC) blocker (IC50 = 2 μM in rat pancreatic β-cells)[1], which is also a blocker of swelling-induced chloride current (ICl, swell) in various cardiovascular tissues (IC50 = 4.1 μM in CPAE cells)[2].?
In intact β-cells, DCPIB inhibits glucose-stimulated insulin secretion through VSAC inhibition and indirect KATP channel activation. DCPIB reverses the shortened duration of action potential induced by cell swelling in atrial myocytes and inhibits astrocyte swelling in vitro. DCPIB (10 μM) also activates TREK1 and TRAAK K+ channels and inhibits TRESK, TASK1 and TASK3 K+ channels in vitro[3].?
References:
[1]. Best L, Yates A P, Decher N, et al. Inhibition of glucose-induced electrical activity in rat pancreatic β-cells by DCPIB, a selective inhibitor of volume-sensitive anion currents. european journal of pharmacology, 2004, 489(1-2): 13-19.
[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, 134(7): 1467-79.
[3]. Lv J, et al. DCPIB, an Inhibitor of Volume-Regulated Anion Channels, Distinctly Modulates K2P Channels. ACS Chem Neurosci, 2019.
- 1. Yuman Wang, Zaiqiao Sun, et al. "Cell volume controlled by LRRC8A-formed volume-regulated anion channels fine-tunes T cell activation and function." Nat Commun. 2023 Nov 4;14(1):7075. PMID: 37925509
- 2. Xiao-yan Wu, Jin-yan Lv, et al. "ML365 inhibits TWIK2 channel to block ATP-induced NLRP3 inflammasome." Acta Pharmacol Sin. 2022 Apr;43(4):992-1000. PMID:34341510
| Physical Appearance | White solid |
| Storage | Store at -20°C |
| M.Wt | 427.37 |
| Cas No. | 82749-70-0 |
| Formula | C22H28Cl2O4 |
| Solubility | insoluble in H2O; ≥49.8 mg/mL in EtOH; ≥50.8 mg/mL in DMSO |
| Chemical Name | 4-((2-butyl-6,7-dichloro-2-cyclopentyl-1-oxo-2,3-dihydro-1H-inden-5-yl)oxy)butanoic acid |
| SDF | Download SDF |
| Canonical SMILES | ClC(C1=C(C=C2OCCCC(O)=O)CC(CCCC)(C1=O)C3CCCC3)=C2Cl |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
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