VU0134992
Based on 4 publication(s) in Google Scholar
VU0134992 is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV.
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- Pureza: 99.30%
- No. CAS: 755002-90-5
- Fòrmula: C20H31BrN2O2
- Peso molecular:411.38
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) VU0134992
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Actividad biológica
IC50: 0.97 µM (Kir4.1)[1]
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[1]. The selectivity of VU0134992 for Kir4.1 versus nine other members of the Kir channel family was evaluated at concentrations ranging from 0.3 nM to 30 µM in 11-point CRC experiments, using established Tl+ flux assays. VU0134992 inhibits 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 at 30 µM, IC50=8.1 µM) with approximately the same efficacy and potency that VU0134992 inhibits Kir4.1 (100% at 30 µM, IC50=5.2 µM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (250-300 g)[1]
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Dosage:50 and 100 mg/kg
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Administration:Oral gavage
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Result:Statistically significantly increased urinary Na+ as well as K+ excretion
Chemical Information
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No. CAS 755002-90-5
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Appearance Solid
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Peso molecular 411.38
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Fòrmula C20H31BrN2O2
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Color White to off-white
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SMILES
O=C(NC1CC(C)(C)NC(C)(C)C1)COC2=CC=C(C(C)C)C=C2Br
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Commun
Activated astrocytes attenuate neocortical seizures in rodent models through driving Na+-K+-ATPase. [Abstract]2022 Nov 21;13(1):7136. PMID: 36414629 -
Glia
2021 Oct;69(10):2474-2487. PMID: 34152032 -
Biochim Biophys Acta Mol Basis Dis
Involvement of Kir4.1 in pain insensitivity of the BTBR mouse model of autism spectrum disorder. [Abstract]2023 Mar 28;1869(5):166700. PMID: 36990129 -
Int J Cancer
High potassium enhances the immunosuppressive function of myeloid-derived suppressor cells via Kir4.1-dependent metabolic reprogramming and promotes tumor immune escape. [Abstract]2025 Dec 29. PMID: 41460024
Pureza y Documentación
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Ficha de datos (271 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VU0134992 Related Classifications
HY-122560 Related Classifications
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