Powder: -20°C for 3 years | In solvent: -80°C for 1 year
VU0134992 hydrochloride is the first subtype-preferring, orally active and selective blocker of Kir4.1 potassium channel pore(IC50 : 0.97 μM).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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2 mg | 在庫あり | ¥ 8,000 | |||
5 mg | 在庫あり | ¥ 13,000 | |||
10 mg | 在庫あり | ¥ 22,500 | |||
25 mg | 在庫あり | ¥ 42,000 | |||
50 mg | 在庫あり | ¥ 72,000 | |||
100 mg | 在庫あり | ¥ 122,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 14,000 |
説明 | 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. |
動物実験 | VU0134992 hydrochloride (250-300 g Male Sprague-Dawley rats;50 and 100 mg/kg) Oral gavage |
分子量 | 447.84 |
分子式 | C20H32BrClN2O2 |
CAS No. | 1052515-91-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 230 mg/mL (513.58 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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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