Furosemide 是 Na+/K+/2Cl- (NKCC

Furosemide  (Synonyms: 呋塞米)

Furosemide 是 Na⁺/K⁺/2Cl^- (NKCC)，NKCC1 和 NKCC2 共转运蛋白的有效的和具有口服活性抑制剂。Furosemide 也是 GABA_A 受体拮抗剂，对含 α6 受体的选择性是含 α1 受体的 100 倍。Furosemide 用作利尿试剂，用于充血性心力衰竭，高血压和水肿的研究。

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
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生物活性    
Furosemide is a potent and orally active inhibitor of Na+/K+/2Cl- (NKCC) cotransporter, NKCC1 and NKCC2[1]. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema[2].

IC50 & Target    
IC50: NKCC1 and NKCC2
IC50: GABAA receptors

体外研究
(In Vitro)    
Furosemide (500 µM; 72-96 hours) significantly changes the proliferation rates in MKN45 cells (the poorly differentiated human gastric adenocarcinoma cell line). however, it has no effects on MKN28 cells (the moderately differentiated human gastric adenocarcinoma cell line). The growth rate of MKN45 cells is larger than that of MKN28 cells[4].
Furosemide (10 µM, 30 µM, 100 µM; 45 min exposure) significantly decreases cation channel activity and [Ca(2+)](i) in human erythrocytes drawn from healthy individuals. Tert-butylhydroperoxide similarly enhances the non-selective cation channels activity, increases [Ca(2+)](i) and triggered cell membrane scrambling, however, the effects is significantly blunted by furosemide again[5].

体内研究
(In Vivo)    
Furosemide (intraperitoneal injection; 100 mg/kg; single dose) is injected after kanamycin (KM) (1000 mg/kg) to creat a deaf mouse model in C57BL/6 mouse. After injection, hearing loss and cochlear hair cell damage are evaluated on day 1, day 2 and day 3, respectively. The hearing is markedly deteriorated even from the next day (Day-1 group), OHCs (outer hair cell) morphology of apical, middle and basal turns are disorganized in mice on day3[3].

分子量    
330.74

性状    
Solid

Formula    
C12H11ClN2O5S

CAS 号    
54-31-9

中文名称    
呋塞米；呋喃苯胺酸；速尿；利尿磺胺；速尿灵

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 (302.35 mM)

H2O : 0.1 mg/mL (0.30 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备液    
浓度溶剂体积质量    1 mg    5 mg    10 mg
1 mM    3.0235 mL    15.1176 mL    30.2352 mL
5 mM    0.6047 mL    3.0235 mL    6.0470 mL
10 mM    0.3024 mL    1.5118 mL    3.0235 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 (7.56 mM); Clear solution

2.
请依序添加每种溶剂： 10% DMSO    90% corn oil

Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution