Home Tools
Log in
Cart

VU0134992 hydrochloride

Catalog No. T13316   CAS 1052515-91-9

VU0134992 hydrochloride is the first subtype-preferring, orally active and selective blocker of Kir4.1 potassium channel pore(IC50 : 0.97 μM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
VU0134992 hydrochloride Chemical Structure
VU0134992 hydrochloride, CAS 1052515-91-9
Pack Size Availability Price/USD Quantity
2 mg In stock $ 34.00
5 mg In stock $ 55.00
10 mg In stock $ 98.00
25 mg In stock $ 183.00
50 mg In stock $ 312.00
100 mg In stock $ 531.00
1 mL * 10 mM (in DMSO) In stock $ 61.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 100%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description VU0134992 hydrochloride is the first subtype-preferring, orally active and selective blocker of 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

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

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

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Orally Active Compound Library Ion Channel Inhibitor Library Anti-Cancer Compound Library Potassium Channel Blocker Library NO PAINS Compound Library Bioactive Compounds Library Max

Related Products

Related compounds with same targets
Cisapride Dequalinium chloride (-)-Denudatin B Pantoprazole Sodium Hydrate Hydroxyhexamide Tolbutamide Flufenamic acid Senicapoc

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

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.

Keywords

VU0134992 hydrochloride 1052515-91-9 Membrane transporter/Ion channel Potassium Channel VU0134992 oral hypertension patch-clamp electrophysiology Kir4.1 VU 0134992 Inhibitor natriuresis inhibit VU-0134992 hydrochloride whole-cell VU-0134992 Hydrochloride VU0134992 Hydrochloride selective kaliuresis VU 0134992 Hydrochloride KcsA VU-0134992 diuresis inhibitor

 

TargetMol