布美他尼 (Ro 10-6338; PF 1593) 是一种高效的袢利尿剂，是一种 Na+-K+-Cl+ 协同转运蛋白 (NKCC) 阻滞剂。
| Cas No. | 28395-03-1 |
| 别名 | 布美他尼; Ro 10-6338; PF 1593 |
| 化学名 | 3-(butylamino)-4-phenoxy-5-sulfamoylbenzoic acid |
| Canonical SMILES | CCCCNC1=C(C(=CC(=C1)C(=O)O)S(=O)(=O)N)OC2=CC=CC=C2 |
| 分子式 | C17H20N2O5S |
| 分子量 | 364.42 |
| 溶解度 | ≥ 18.221mg/mL in DMSO |
| 储存条件 | 4°C, protect from light |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Bumetanide (Ro 10-6338;PF 1593) is a selective Na+-K+-Cl- cotransporter 1 (NKCC1) inhibitor, weakly inhibits NKCC2, with IC50s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively[4]. References:
[1]. Frelin C, et al. Biochemical characterization of the Na+/K+/Cl- co-transport in chick cardiac cells. Biochem Biophys Res Commun. 1986 Jan 14;134(1):326-31.
[2]. 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.
[3]. Bourrit A, et al. Basic characterization of an ouabain-resistant, bumetanide-sensitive K+ carrier-mediated transport system in J774.2 mouse macrophage-like cell line and in variants deficient in adenylate cyclase and cAMP-dependent protein kinase activities. Biochim Biophys Acta. 1985 Jul 11;817(1):85-94.
[4]. Sandstr m PE. Evidence for diabetogenic action of bumetanide in mice. Eur J Pharmacol. 1988 May 20;150(1-2):35-41. |
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