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VU0134992 hydrochloride
Catalog No. T13316Cas No. 1052515-91-9
VU0134992 hydrochloride is the first subtype-preferring, orally active and selective blocker of the Kir4.1 potassium channel pore (IC50: 0.97 μM).
VU0134992 hydrochloride
Catalog No. T13316Cas No. 1052515-91-9
VU0134992 hydrochloride is the first subtype-preferring, orally active and selective blocker of the Kir4.1 potassium channel pore (IC50: 0.97 μM).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $34 | In Stock | |
| 5 mg | $55 | In Stock | |
| 10 mg | $98 | In Stock | |
| 25 mg | $183 | In Stock | |
| 50 mg | $312 | In Stock | |
| 100 mg | $531 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $61 | In Stock |
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Purity:100%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | VU0134992 hydrochloride is the first subtype-preferring, orally active and selective blocker of the Kir4.1 potassium channel pore (IC50: 0.97 μM). |
| In vitro | In whole-cell patch-clamp electrophysiology experiments, VU0134992 inhibits Kir4.1 with an IC50 value of 0.97 M and is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50 = 9 M) at -120 mV. In thallium (Tl+) flux assays, VU0134992 is greater than 30-fold selective for Kir4.1 over Kir1.1, Kir2.1, and Kir2.2; is weakly active toward Kir2.3, Kir6.2/SUR1, and Kir7.1; and is equally active toward Kir3.1/3.2, Kir3.1/3.4, and Kir4.2. This potency and selectivity profile is superior to Kir4.1 inhibitors amitriptyline, nortriptyline, and fluoxetine. Medicinal chemistry identified components of VU0134992 that are critical for inhibiting Kir4.1. Patch-clamp electrophysiology, molecular modeling, and site-directed mutagenesis identified pore-lining glutamate 158 and isoleucine 159 as critical residues for block of the channel. |
| In vivo | VU0134992 displayed a large free unbound fraction (fu) in rat plasma (fu = 0.213).Consistent with the known role of Kir4.1 in renal function, oral dosing of VU0134992 led to a dose-dependent diuresis, natriuresis, and kaliuresis in rats.Thus, VU0134992 represents the first in vivo active tool compound for probing the therapeutic potential of Kir4.1 as a novel diuretic target for the treatment of hypertension. |
| Animal Research | VU0134992 hydrochloride (250-300 g Male Sprague-Dawley rats;50 and 100 mg/kg) Oral gavage |
| Molecular Weight | 447.84 |
| Formula | C20H32BrClN2O2 |
| Cas No. | 1052515-91-9 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 230 mg/mL (513.58 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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