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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- Purity : 99.30%
- CAS No.: 755002-90-5
- 화학식: C20H31BrN2O2
- 분자량:411.38
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) VU0134992
More
Biological Activity
제품 설명
IC50 & Target
IC50: 0.97 µM (Kir4.1)[1]
In Vitro
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. .
In Vivo
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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CAS No. 755002-90-5
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Appearance Solid
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분자량 411.38
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
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
순도&문서
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Data Sheet (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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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VU0134992 Related Classifications
HY-122560 Related Classifications
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