| 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 |
Kir4.1 (inward-rectifier potassium channel).
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| ln Vitro |
More than thirty times as selective as Kir1.1, Kir2.1, and Kir2.2, VU0134992 exhibits weak activity against Kir2.3, Kir6.2/SUR1, and Kir7.1, and exhibits the same activity against Kir7.1 as Kir3.1/3.2, Kir3.1/3.4, and Kir4.2[1]. An established Tl+ flux assay was used in an 11-point CRC experiment to assess the selectivity of VU0134992 for Kir4.1 against nine other members of the Kir channel family over a dose range of 0.3 nM to 30 µM. Approximately the same efficacy and potency as VU0134992 in inhibiting Kir4.1 (100%, 30 µM, IC50=5.2 µM) is observed in the inhibition of Kir3.1/Kir3.2 (92% inhibition at 30 µM, IC50=2.5 µM), Kir3.1/Kir3.4 (92% inhibition at 30 µM, IC50=3.1 µM), and Kir4.2 (100% Inhibition (30 µM, IC50=8.1 µM) [1].
VU0134992 is a potent Kir4.1 blocker with an IC50 of 0.97 μM. It is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV, representing the first in vivo-active tool compound for probing Kir4.1 therapeutic potential. |
| ln Vivo |
Urinary Na+ and K+ excretion are statistically significantly increased by VU0134992 (50-100 mg/kg; oral gavage) [1].
No detailed in vivo activity data is available beyond its characterization as an orally active compound. Studies have evaluated its effects on renal fluid and electrolyte excretion, consistent with its potential as a diuretic target. |
| Enzyme Assay |
The compound's Kir4.1 blocking activity is assessed in cell-free systems using electrophysiological techniques such as patch-clamp recording on excised membrane patches containing Kir4.1 channels. These assays measure the compound's ability to block potassium current through the channel pore.
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| Cell Assay |
VU0134992 is evaluated in cell-based assays using patch-clamp electrophysiology on cells expressing homomeric Kir4.1 or Kir4.1/5.1 concatemeric channels. The compound shows an IC50 of 0.97 μM for Kir4.1 and 9 µM for Kir4.1/5.1 at -120 mV.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (250-300 g) [1]
Doses: 50 and 100 mg/kg Route of Administration: po (oral gavage) Experimental Results: Significant increase in urinary Na+ and K+ excretion In vivo studies are conducted in male Sprague-Dawley rats (250-300 g) to evaluate the compound's effects on renal fluid and electrolyte excretion. Doses of 50 and 100 mg/kg are administered to assess diuretic efficacy and mechanism of action. |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is available for VU0134992. As an orally active compound, it is expected to have sufficient oral bioavailability for in vivo studies, but 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 tool compound, standard preclinical toxicity assessments have not been published.
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| References |
[1]. Kharade SV, et al. Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992. Mol Pharmacol. 2018 Aug;94(2):926-937.
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| Additional Infomation |
VU0134992 has a molecular formula of C20H31BrN2O2 and a molecular weight of 411.38. The compound is the first in vivo-active tool compound for probing Kir4.1 as a novel diuretic target for hypertension treatment. It has not advanced to clinical trials and is not FDA-approved.
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| Molecular Formula |
C20H31BRN2O2
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|---|---|
| Molecular Weight |
411.376344919205
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| Exact Mass |
410.156
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| CAS # |
755002-90-5
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| Related CAS # |
VU0134992 hydrochloride;1052515-91-9
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| PubChem CID |
1319582
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
449
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)C1=CC(=C(C=C1)OCC(=O)NC2CC(NC(C2)(C)C)(C)C)Br
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| InChi Key |
OTTDLWFVHQYRDA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H31BrN2O2/c1-13(2)14-7-8-17(16(21)9-14)25-12-18(24)22-15-10-19(3,4)23-20(5,6)11-15/h7-9,13,15,23H,10-12H2,1-6H3,(H,22,24)
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| Chemical Name |
2-(2-Bromo-4-isopropylphenoxy)-N-(2,2,6,6-tetramethylpiperidin-4-yl)acetamide
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| Synonyms |
VU-992 VU 992 VU992 VU-0134992 VU 0134992 VU0134992
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.4308 mL | 12.1542 mL | 24.3084 mL | |
| 5 mM | 0.4862 mL | 2.4308 mL | 4.8617 mL | |
| 10 mM | 0.2431 mL | 1.2154 mL | 2.4308 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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