ChemicalBook--->CAS DataBase List--->1052515-91-9

1052515-91-9

1052515-91-9 Structure

1052515-91-9 Structure
IdentificationBack Directory
[Name]

VU0134992(hydrochloride)
[CAS]

1052515-91-9
[Synonyms]

VU0134992(hydrochloride)
[Molecular Formula]

C20H32BrClN2O2
[MDL Number]

MFCD05985784
[MOL File]

1052515-91-9.mol
[Molecular Weight]

447.84
Chemical PropertiesBack Directory
[storage temp. ]

Inert atmosphere,2-8°C
[solubility ]

DMSO: 2mg/mL, clear
[form ]

Solid
[color ]

White to off-white
[InChIKey]

QXKQUPCNSXWIDX-UHFFFAOYSA-N
[SMILES]

CC(C)C1=CC(Br)=C(OCC(NC2CC(C)(C)NC(C)(C)C2)=O)C=C1.Cl
Safety DataBack Directory
[Symbol(GHS) ]

Exclamation Mark (GHS07)
GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P280-P301+P312-P302+P352-P305+P351+P338
[WGK Germany ]

WGK 3
[Storage Class]

11 - Combustible Solids
Hazard InformationBack Directory
[Uses]

VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 μM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 μM) at -120 mV[1].
[Biological Activity]

VU0134992 is an orally availablepotent and selective modulator of the inward rectifier potassium (Kir) channel Kir4.1 (KCNJ10) th at induces diuresisnatriuresisand kaliuresis in rats.
[in vivo]

VU0134992 hydrochloride (50-100 mg/kg; oral gavage) statistically significantly increased urinary Na+ as well as K+ excretion[1].

Animal Model:Male Sprague-Dawley rats (250-300 g)[1]
Dosage:Oral gavage
Administration:50 and 100 mg/kg
Result:Statistically significantly increased urinary Na+ as well as K+ excretion.
[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. DOI:10.1124/mol.118.112359
Spectrum DetailBack Directory
[Spectrum Detail]

VU0134992(hydrochloride)(1052515-91-9)1HNMR
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