1222810-74-3
Chemical Structure
VU591
- CAS No.: 1222810-74-3
- Formula:C16H12N6O5
- Molecular Weight:368.30
IUPAC Name: 2,2'-(oxybis(methylene))bis(6-nitro-1H-benzo[d]imidazole)
InChIKey: ZQPXNYLXYNRFNP-UHFFFAOYSA-N
SMILES: O=[N+]([O-])C1=CC(NC(COCC2=NC3=C(N2)C=C([N+]([O-])=O)C=C3)=N4)=C4C=C1
Biological Activity: VU591 is a selective inhibitor of the renal outer medullary potassium channel (ROMK, Kir1.1). VU591 inhibits ROMK via binding to the intracellular pore region near residues Val168 and Asn171, with IC50 of 240 nM in Tl+ flux assay and 300 nM in whole cell patch clamp electrophysiology, suppresses native ROMK mediated K+ secretion in isolated perfused rat collecting ducts, and exerts antidepressive effects in the mouse tail suspension test (TST). VU591 can be used for the study of ROMK channel function, renal potassium handling, antidepressant mechanisms, and diuretic drug discovery[1][2][3][4][5].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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VU591 | 98.81% | VU591 is a selective inhibitor of the renal outer medullary potassium channel (ROMK, Kir1.1). VU591 inhibits ROMK via binding to the intracellular pore region near residues Val168 and Asn171, with IC50 of 240 nM in Tl+ flux assay and 300 nM in whole cell patch clamp electrophysiology, suppresses native ROMK mediated K+ secretion in isolated perfused rat collecting ducts, and exerts antidepressive effects in the mouse tail suspension test (TST). VU591 can be used for the study of ROMK channel function, renal potassium handling, antidepressant mechanisms, and diuretic drug discovery. | ||||||||||||||||||||
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- [1]. Bhave G, et al. Development of a selective small-molecule inhibitor of Kir1.1, the renal outer medullary potassium channel. Mol Pharmacol. 2011 Jan;79(1):42-50. [Content Brief]
- [2]. Okada M, et al. Antidepressive effect of an inward rectifier K+ channel blocker peptide, tertiapin-RQ. PLoS One. 2020 Nov 13;15(11):e0233815. [Content Brief]
- [3]. Swale DR, et al. Computational and functional analyses of a small-molecule binding site in ROMK. Biophys J. 2015 Mar 10;108(5):1094-103. [Content Brief]
- [4]. Sammons MF, et al. Discovery and in Vitro Optimization of 3-Sulfamoylbenzamides as ROMK Inhibitors. ACS Med Chem Lett. 2018 Jan 19;9(2):125-130. [Content Brief]
- [5]. Wang J, et al. Kir1.1 and SUR1 are not implicated as subunits of an adenosine triphosphate-sensitive potassium channel involved in diazoxide cardioprotection. JTCVS Open. 2023 Jun 16;15:231-241. [Content Brief]
Keywords
