| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
ROMK (renal outer medullary potassium channel, Kir1.1).
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|---|---|
| ln Vitro |
VU591 is a ROMK channel pore blocker and selective ROMK inhibitor. In addition to having strong metabolic stability, VU591 can bind to serum proteins [1].
VU591 is a potent, selective ROMK inhibitor with an IC50 of 0.24 μM in flux assays. It blocks the intracellular pore of the channel and does not inhibit Kir7.1 (unlike the related compound VU590). |
| ln Vivo |
In TST, VU591 (icv; 1.842 μg) dramatically reduces immobility time [2].
No detailed in vivo activity data is available for this compound. As a ROMK inhibitor with diuretic potential, it is expected to have effects on renal electrolyte excretion and blood pressure, but specific in vivo studies have not been reported. |
| Enzyme Assay |
The compound's ROMK inhibitory activity is assessed in cell-free systems using membrane preparations from cells expressing ROMK channels. Flux assays or electrophysiological recordings measure the compound's ability to block potassium flux through the channel pore.
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| Cell Assay |
VU591 is evaluated in cell-based assays using cells expressing ROMK (Kir1.1) channels. Flux assays or patch-clamp electrophysiology measure the compound's ability to inhibit potassium currents, with an IC50 of 0.24 μM.
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| Animal Protocol |
Animal/Disease Models: Male ICR mouse [2]
Doses: 1.842 μg Route of Administration: icv; 1.842 μg; Experimental Results:demonstrated antidepressant effect in tail suspension test (TST). No detailed in vivo animal experimental protocol is available for this compound. For ROMK inhibitors, typical in vivo studies involve rodent models to assess diuretic efficacy, electrolyte excretion, and blood pressure effects. |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is available for VU591. With a molecular weight of approximately 380, specific PK parameters have not been reported.
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| Toxicity/Toxicokinetics |
No detailed toxicological data is available for this compound. As a research-grade chemical probe, standard preclinical toxicity assessments have not been published.
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| References | |
| Additional Infomation |
VU591 has a molecular formula of C16H12N6O5. The compound is a potent, selective ROMK inhibitor that serves as a useful probe to explore the viability of ROMK as a diuretic target for lowering blood volume and pressure without causing hypokalemia. It has not advanced to clinical trials and is not FDA-approved.
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| Molecular Formula |
C16H12N6O5
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|---|---|
| Molecular Weight |
368.3
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| Exact Mass |
368.087
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| CAS # |
1222810-74-3
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| Related CAS # |
VU591 hydrochloride;1315380-70-1
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| PubChem CID |
44123657
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.018
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
521
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| Defined Atom Stereocenter Count |
0
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| Synonyms |
VU 591 VU-591 VU591
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~62.5 mg/mL (~169.70 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.65 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7152 mL | 13.5759 mL | 27.1518 mL | |
| 5 mM | 0.5430 mL | 2.7152 mL | 5.4304 mL | |
| 10 mM | 0.2715 mL | 1.3576 mL | 2.7152 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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