CAS號(hào)	28395-03-1	產(chǎn)地	國產(chǎn)
規(guī)格	500mg	級(jí)別	化工級(jí)
證書	ISO系列證書

Bumetanide (Synonyms: 布美她尼; Ro 10-6338; PF 1593)

Bumetanide (Ro 10-6338; PF 1593) 是一種高效的li尿劑，是 Na⁺-K⁺-Cl⁺ 協(xié)同轉(zhuǎn)運(yùn)蛋白 (NKCC) 的阻斷劑。Bumetanide 是選擇性的 NKCC1 抑制劑，但對(duì) NKCC2 也有抑制作用，對(duì) hNKCC1A 和 hNKCC2A 作用的 IC₅₀ 值分別為 0.68 μM 和 4.0 μM。

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

IC₅₀ & Target

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

體外研究(In Vitro)

Bumetanide has inhibitory effects for the two major human splice variants of NKCCs, hNKCC1A and hNKCC2A ^[1].
Bumetanide (0.03-100 μM; 5 minutes) inhibits the ⁸⁶Rb⁺ uptake in NKCC1A-expressing oocytes in a dose-dependent manner^[1].
Bumetanide inhibits NKCC2 isoform B in HEK-293 cells with an IC₅₀ value of 0.54 μM

體內(nèi)研究(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^[3].
Bumetanide also reduces infarct size^[3].
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

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).

Animal Model:	Male Sprague-Dawley rats (220-300 g)^[4]
Dosage:	2 mg/kg, 8 mg/kg, 20 mg/kg (Pharmacokinetic Analysis)
Administration:	Intravenous administration
Result:	T_1/2 (21.4 min, 53.8 min and 137 min for 2 mg/kg, 8 mg/kg and 20 mg/kg, respectively )

分子量：364.42

Formula：C₁₇H₂₀N₂O₅S

CAS 號(hào)：28395-03-1

中文名稱：布美她尼；5-正丁氨基-4-苯氧基-3-氨基磺?；郊姿?；3-(氨基磺酰基)-5-(丁基氨基)-4-苯氧基苯甲酸；3-正丁胺基-4苯氧基-5-氨基磺酰苯甲酸

運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

4°C, protect from light

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

溶解性數(shù)據(jù)

DMSO : 100 mg/mL (274.41 mM; Need ultrasonic)

H₂O : 0.1 mg/mL (0.27 mM; Need ultrasonic)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)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

請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution
2.

請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

參考文獻(xiàn)

[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.

[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.

[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.

[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

注：產(chǎn)品僅用于科研