Bumetanide布美他尼,28395-03-1

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Bumetanide

CAS No. : 28395-03-1

MCE 国际站：Bumetanide

产品活性：Bumetanide (Ro 10-6338; PF 1593) 是一种高效的利尿剂，是 Na⁺-K⁺-Cl⁺ 协同转运蛋白 (NKCC) 的阻断剂。Bumetanide 是选择性的 NKCC1 抑制剂，但对 NKCC2 也有抑制作用，对 hNKCC1A 和 hNKCC2A 作用的 IC₅₀ 值分别为 0.68 μM 和 4.0 μM。

研究领域：Membrane Transporter/Ion Channel

作用靶点：NKCC

In Vitro: Bumetanide has inhibitory effects for the two major human splice variants of NKCCs, hNKCC1A, and hNKCC2A .
Bumetanide (0.03-100 μM; 5 minutes) inhibits the ⁸⁶Rb⁺ uptake in NKCC1A-expressing oocytes in a dose-dependent manner.
Bumetanide inhibits NKCC2 isoform B in HEK-293 cells with an IC₅₀ value of 0.54 μM.

In Vivo: Bumetanide (7.6-30.4 mg/kg; i.v.) attenuates the decrease in apparent diffusion coefficients (ADC) ratios for both cortex and striatum (by 40-67%), indicating reduced edema formation.
Bumetanide also reduces infarct size.
Bumetanide shows different half-lives of 21.4 min, 53.8 min, and 137 min following 2 mg/kg, 8 mg/kg, and 20 mg/kg intravenous injection, respectively, in rats.

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