文献支持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。

价格： ￥500

品牌：medchemexpress(MCE)

货号：HY-17468

产品详情

Bumetanide (Synonyms: 布美他尼; Ro 10-6338; PF 1593)

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。

美国medchemexpress（MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
MCE中国是全球领先的科研化学品和生物活性化合物供应商，总部位于美国新泽西。我们的产品范围覆盖各种抑制剂、激动剂、API和化合物库。专业、高效的企业灵魂铸造了在行业的卓越地位。热情和充满活力的研发团队拥有着大量的化学和生物科学家。专注于生物活性化合物，拥有着多年的发展历程和丰富的行业经验。

生物活性
Bumetanide (Ro 10-6338; PF 1593), a highly potent loop diuretic, is a Na+-K+-Cl+ cotransporter (NKCC) blocker. Bumetanide is a selective NKCC1 inhibitor, but also inhibits NKCC2, with IC50s of 0.68 μM and 4.0 μM for hNKCC1A and hNKCC2A, respectively[1][2].

IC50 & Target
IC50: 0.68 μM (hNKCC1A), 4.0 μM (hNKCC2A)[1]

体外研究(In Vitro)
Bumetanide 对人类 NKCC 的两种主要剪接变体 hNKCC1A 和 hNKCC2A 具有抑制作用[1]。
Bumetanide (0.03-100 μM；5 分钟) 抑制86Rb+ 在表达 NKCC1A 的卵母细胞中以剂量依赖性方式摄取[1]。
Bumetanide 抑制 HEK-293 细胞中的 NKCC2 亚型 B，具有 IC50 值为 0.54 μM[2]。

体内研究(In Vivo)
Bumetanide (7.6-30.4 mg/kg；静脉注射) 减弱了皮质和纹状体表观扩散系数 (ADC) 比率的降低 (降低了 40-67%)，表明水肿形成减少[3]。
Bumetanide 还可以减少梗塞面积[3]。
Bumetanide 在 2 mg/kg、8 mg/kg 和大鼠分别静脉注射 20 mg/kg[4]。

Animal Model:   Normotensive Sprague-Dawley rats (250-300 g)[3]
Dosage:   7.6 mg/kg, 15.2 mg/kg, 30.4 mg/kg
Administration:   Intravenous injection
Result:   Reduced the middle cerebral artery occlusion (MCAO)-induced decrease in ADC values in all four ipsilateral regions (L1-L4).

分子量
364.42

性状
Solid

Formula
C17H20N2O5S

CAS 号
28395-03-1

中文名称
布美他尼；强力速效利尿剂

运输条件
Room temperature in continental US; may vary elsewhere.

储存方式
4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro:
DMSO : 100 mg/mL (274.41 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (ultrasonic) (insoluble)

配制储备液
浓度溶剂体积质量   1 mg   5 mg   10 mg
1 mM   2.7441 mL   13.7204 mL   27.4409 mL
5 mM   0.5488 mL   2.7441 mL   5.4882 mL
10 mM   0.2744 mL   1.3720 mL   2.7441 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

2.
请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

参考文献	[1]. Lykke K, et al. The search for NKCC1-selective drugs for the treatment of epilepsy: Structure-function relationship of bumetanide and various bumetanide derivatives in inhibiting the human cation-chloride cotransporter NKCC1A. Epilepsy Behav. 2016 Jun;59:42-9. [Content Brief] [2]. Ciaran Richardson, et al. Regulation of the NKCC2 ion cotransporter by SPAK-OSR1-dependent and -independent pathways. J Cell Sci. 2011 Mar 1;124(Pt 5):789-800. [Content Brief] [3]. Martha E O'Donnell, et al. Bumetanide inhibition of the blood-brain barrier Na-K-Cl cotransporter reduces edema formation in the rat middle cerebral artery occlusion model of stroke. J Cereb Blood Flow Metab. 2004 Sep;24(9):1046-56. [Content Brief] [4]. S H Lee, et al. Pharmacokinetics and pharmacodynamics of bumetanide after intravenous and oral administration to rats: absorption from various GI segments. J Pharmacokinet Biopharm. 1994 Feb;22(1):1-17.6 [Content Brief]

参考文献

[1]. Lykke K, et al. The search for NKCC1-selective drugs for the treatment of epilepsy: Structure-function relationship of bumetanide and various bumetanide derivatives in inhibiting the human cation-chloride cotransporter NKCC1A. Epilepsy Behav. 2016 Jun;59:42-9.  [Content Brief]

[2]. Ciaran Richardson, et al. Regulation of the NKCC2 ion cotransporter by SPAK-OSR1-dependent and -independent pathways. J Cell Sci. 2011 Mar 1;124(Pt 5):789-800.  [Content Brief]

[3]. Martha E O'Donnell, et al. Bumetanide inhibition of the blood-brain barrier Na-K-Cl cotransporter reduces edema formation in the rat middle cerebral artery occlusion model of stroke. J Cereb Blood Flow Metab. 2004 Sep;24(9):1046-56.  [Content Brief]

[4]. S H Lee, et al. Pharmacokinetics and pharmacodynamics of bumetanide after intravenous and oral administration to rats: absorption from various GI segments. J Pharmacokinet Biopharm. 1994 Feb;22(1):1-17.6  [Content Brief]

参考文献	[1]. Lykke K, et al. The search for NKCC1-selective drugs for the treatment of epilepsy: Structure-function relationship of bumetanide and various bumetanide derivatives in inhibiting the human cation-chloride cotransporter NKCC1A. Epilepsy Behav. 2016 Jun;59:42-9. [Content Brief] [2]. Ciaran Richardson, et al. Regulation of the NKCC2 ion cotransporter by SPAK-OSR1-dependent and -independent pathways. J Cell Sci. 2011 Mar 1;124(Pt 5):789-800. [Content Brief] [3]. Martha E O'Donnell, et al. Bumetanide inhibition of the blood-brain barrier Na-K-Cl cotransporter reduces edema formation in the rat middle cerebral artery occlusion model of stroke. J Cereb Blood Flow Metab. 2004 Sep;24(9):1046-56. [Content Brief] [4]. S H Lee, et al. Pharmacokinetics and pharmacodynamics of bumetanide after intravenous and oral administration to rats: absorption from various GI segments. J Pharmacokinet Biopharm. 1994 Feb;22(1):1-17.6 [Content Brief]