| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
VU590 targets the renal outer medullary potassium channel (ROMK, Kir1.1), an inward rectifier potassium channel expressed in the kidney that plays a critical role in potassium homeostasis and renal function. VU590 also inhibits Kir7.1, an inward rectifying potassium channel. VU590 modulates uterine myometrial contractility and melanocortin signaling.
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| ln Vitro |
In vitro, VU590 is a potent and moderately selective ROMK inhibitor with an IC₅₀ of 290 nM. It shows significant inhibitory activity against rat ROMK1 in HEK293 cells with an IC₅₀ of 294 nM. VU590 also inhibits human Kir7.1 with 69% inhibition at 10 µM. VU590 is not a good probe of ROMK function in the kidney.
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| ln Vivo |
In vivo, VU590 modulates uterine myometrial contractility and melanocortin signaling. As a ROMK inhibitor, it may affect renal potassium handling and blood pressure regulation. Detailed in vivo data regarding dosage, administration routes, and specific efficacy endpoints are limited in the available literature.
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| Enzyme Assay |
VU590's potassium channel inhibition activity has been characterized using electrophysiological techniques such as patch clamp assays. The compound inhibits ROMK (Kir1.1) with an IC₅₀ of 290 nM and Kir7.1 with an IC₅₀ of 8 μM. Binding and functional assays are performed using cells expressing the target channels.
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| Cell Assay |
In vitro cell experiments with VU590 typically use HEK293 cells expressing ROMK1 or Kir7.1 channels. Cells are treated with the compound at various concentrations, and channel activity is measured using patch clamp electrophysiology or thallium flux assays. The compound's effects on channel inhibition and selectivity are assessed.
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| Animal Protocol |
In vivo animal studies with VU590 have been conducted to study its effects on uterine myometrial contractility and melanocortin signaling. The compound is typically administered via injection. Detailed protocols regarding dosage, treatment duration, and specific animal models are not extensively reported.
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| ADME/Pharmacokinetics |
Pharmacokinetic data specific to VU590 are limited in the available literature. As a small molecule with a molecular weight of 488.53 g/mol, the compound is expected to have reasonable bioavailability. Further pharmacokinetic studies are needed to fully characterize its absorption, distribution, metabolism, and excretion properties.
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| Toxicity/Toxicokinetics |
VU590 is considered safe for research use at typical concentrations. As a research compound, it is intended for laboratory use only and not for human consumption. The compound should be stored at 4°C, protected from light. Standard laboratory safety practices should be followed.
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| References |
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| Additional Infomation |
VU590 has a molecular formula of C₂₈H₂₈N₄O₃ and a molecular weight of 488.53 g/mol. It is a potent and moderately selective ROMK (Kir1.1) inhibitor with an IC₅₀ of 290 nM and also inhibits Kir7.1 with an IC₅₀ of 8 μM. It is the first small-molecule inhibitor of ROMK and Kir7.1.
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| Molecular Formula |
C24H34CL2N4O7
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|---|---|
| Molecular Weight |
561.455364704132
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| Exact Mass |
560.18
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| CAS # |
313505-85-0
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| PubChem CID |
71433535
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| Appearance |
White to off-white solid powder
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| LogP |
5.396
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
37
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| Complexity |
562
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1COCCN(CCOCCOCCN1CC2=CC=C(C=C2)[N+](=O)[O-])CC3=CC=C(C=C3)[N+](=O)[O-].Cl.Cl
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| InChi Key |
FRYYSUBAHIUBNJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H32N4O7.2ClH/c29-27(30)23-5-1-21(2-6-23)19-25-9-13-33-14-10-26(12-16-35-18-17-34-15-11-25)20-22-3-7-24(8-4-22)28(31)32;;/h1-8H,9-20H2;2*1H
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| Chemical Name |
7,13-bis[(4-nitrophenyl)methyl]-1,4,10-trioxa-7,13-diazacyclopentadecane;dihydrochloride
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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 : ~50 mg/mL (~102.35 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7811 mL | 8.9054 mL | 17.8107 mL | |
| 5 mM | 0.3562 mL | 1.7811 mL | 3.5621 mL | |
| 10 mM | 0.1781 mL | 0.8905 mL | 1.7811 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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