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VU0134992 hydrochloride

Name: VU0134992 hydrochloride
Brand: TargetMol
SKU: T13316
Price: 31 USD
Availability: InStock
Rating: 5 (10 reviews)

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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

🥰Excellent

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	USA Warehouse	Global Warehouse
5 mg	$31	In Stock	In Stock
10 mg	$54	In Stock	In Stock
25 mg	$106	In Stock	In Stock
50 mg	$179	In Stock	In Stock
100 mg	$297	In Stock	In Stock
200 mg	$459	-	In Stock
1 mL x 10 mM (in DMSO)	$35	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Batch Information

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Purity:>99.99%

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COA HNMR LCMS

Product Introduction

Bioactivity

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

Chemical Properties

Molecular Weight	447.84
Formula	C₂₀H₃₂BrClN₂O₂
Cas No.	1052515-91-9
Smiles	Cl.CC(C)c1ccc(OCC(=O)NC2CC(C)(C)NC(C)(C)C2)c(Br)c1
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 230 mg/mL (513.58 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (11.16 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2329 mL	11.1647 mL	22.3294 mL	111.6470 mL
5 mM	0.4466 mL	2.2329 mL	4.4659 mL	22.3294 mL
10 mM	0.2233 mL	1.1165 mL	2.2329 mL	11.1647 mL
20 mM	0.1116 mL	0.5582 mL	1.1165 mL	5.5824 mL
50 mM	0.0447 mL	0.2233 mL	0.4466 mL	2.2329 mL
100 mM	0.0223 mL	0.1116 mL	0.2233 mL	1.1165 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(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 TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc