VU 591 hydrochloride

Selective Kir1.1 (ROMK) inhibitor CAS# 1315380-70-1

VU 591 hydrochloride

2D Structure

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3D structure

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VU 591 hydrochloride

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Chemical Properties of VU 591 hydrochloride

Cas No. 1315380-70-1 SDF Download SDF
PubChem ID 90488918 Appearance Powder
Formula C16H13ClN6O5 M.Wt 404.76
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 16.67 mg/mL (41.18 mM; Need ultrasonic)
Chemical Name 6-nitro-2-[(6-nitro-1H-benzimidazol-2-yl)methoxymethyl]-1H-benzimidazole;hydrochloride
SMILES C1=CC2=C(C=C1[N+](=O)[O-])NC(=N2)COCC3=NC4=C(N3)C=C(C=C4)[N+](=O)[O-].Cl
Standard InChIKey PXLOUHLPDHEXCC-UHFFFAOYSA-N
Standard InChI InChI=1S/C16H12N6O5.ClH/c23-21(24)9-1-3-11-13(5-9)19-15(17-11)7-27-8-16-18-12-4-2-10(22(25)26)6-14(12)20-16;/h1-6H,7-8H2,(H,17,19)(H,18,20);1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of VU 591 hydrochloride

DescriptionSelective renal outer medullary potassium channel (Kir1.1, ROMK) antagonist (IC50 = 300 nM). Thought to block the intracellular pore of the Kir1.1 channel. Exhibits no effect on Kir7.1 at concentrations up to 10 μM; does not inhibit Kir2.1, Kir2.3 or Kir4.1. Displays similar potency to VU 590 .

VU 591 hydrochloride Dilution Calculator

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VU 591 hydrochloride Molarity Calculator

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Preparing Stock Solutions of VU 591 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4706 mL 12.353 mL 24.706 mL 49.412 mL 61.765 mL
5 mM 0.4941 mL 2.4706 mL 4.9412 mL 9.8824 mL 12.353 mL
10 mM 0.2471 mL 1.2353 mL 2.4706 mL 4.9412 mL 6.1765 mL
50 mM 0.0494 mL 0.2471 mL 0.4941 mL 0.9882 mL 1.2353 mL
100 mM 0.0247 mL 0.1235 mL 0.2471 mL 0.4941 mL 0.6176 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on VU 591 hydrochloride

Development of a selective small-molecule inhibitor of Kir1.1, the renal outer medullary potassium channel.[Pubmed:20926757]

Mol Pharmacol. 2011 Jan;79(1):42-50.

The renal outer medullary potassium (K+) channel, ROMK (Kir1.1), is a putative drug target for a novel class of loop diuretic that would lower blood volume and pressure without causing hypokalemia. However, the lack of selective ROMK inhibitors has hindered efforts to assess its therapeutic potential. In a high-throughput screen for small-molecule modulators of ROMK, we previously identified a potent and moderately selective ROMK antagonist, 7,13-bis(4-nitrobenzyl)-1,4,10-trioxa-7,13-diazacyclopentadecane (VU590), that also inhibits Kir7.1. Because ROMK and Kir7.1 are coexpressed in the nephron, VU590 is not a good probe of ROMK function in the kidney. Here we describe the development of the structurally related inhibitor 2,2'-oxybis(methylene)bis(5-nitro-1H-benzo[d]imidazole) (VU591), which is as potent as VU590 but is selective for ROMK over Kir7.1 and more than 65 other potential off-targets. VU591 seems to block the intracellular pore of the channel. The development of VU591 may enable studies to explore the viability of ROMK as a diuretic target.

Description

VU591 hydrochloride is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM.

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