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CAS No.: 127-69-5

磺胺异噁唑 Catalog No. CSN12014

Synonyms: 磺胺异恶唑;Sulfafurazole

Sulfisoxazole is an antagonist of endothelin receptor that can be used as a sulfonamide antibacterial agent.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The endothelins(ET) are a family of potent vasoactive peptides first isolated from the supernatant of cultured porcine aorta cells. Currently, three members of the endothelin family, namely ET-1, 2 and 3, are known. Elevated levels of ET-1 have been found in patients with myocardial infarction, vasospastic angina, cardiogenic and septic shock, sub-arachnoid hemorrhage and renal failure^[3]. Endothelins are formed from the corresponding big endothelins through the action of endothelin converting enzymes. They exert their actions via specific membrane recepters. Two endothelin receptor subtypes have been isolated and cloned^[3]. The sulfanilamide antibacterial agent sulfisoxazole is found to be a good endothelin receptor antagonist (IC50's of 0.60 µM and 22 µM for the ETA and ETB receptors, respectively) ^[3]. ET-1 causes a dose dependent accumulation of phosphoinositide metabolites in TE 671 cells and in the transfected COS 7 cells in the presence of lithium. Addition of sulfisoxazole results in a parallel shift to the right of the ET-1 dose response curve in the TE 671 cells indicating that sulfisoxazole acts as a functional antagonist of ET-1 in this system^[3]. Experimental studies in rats have recently proved that the use of the antagonist protects the retina against ischemic damage in processes like glaucoma, reducing electro-retinogram alterations and normalizing changes in the acetylcolintransferase levels, synthethase nitric oxide, Thy-1(a specific marker of retina ganglionary cells) and FGF-2 (trophic factor produced by glial cells in stress conditions), typical of ischemia conditions^[4].
动物研究
剂量
Rat: 5 mg/kg^[3] (i.p.); 25 mg/kg - 225 mg/kg^[2] (p.o.)

给药途径
i.p., p.o.
临床研究

动物研究
剂量	Rat: 5 mg/kg^[3] (i.p.); 25 mg/kg - 225 mg/kg^[2] (p.o.)
给药途径	i.p., p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02099240	Osteomyelitis	Early Phase 1	Recruiting	September 2019	United States, Kentucky ... more >> University of Louisville Recruiting Louisville, Kentucky, United States, 40202 Contact: Julio A Ramirez, MD 502-852-1148 jarami01@louisville.edu Contact: David Seligson, MD 502-852-0923 d0seli01@louisville.edu Sub-Investigator: Forest Arnold, DO Sub-Investigator: Timothy Wiemkwn, PhD Sub-Investigator: Robert Kelley, PhD Sub-Investigator: James Summersgill, PhD Sub-Investigator: Ruth Carrico, PhD Sub-Investigator: Julie Harting, PharmD Sub-Investigator: Paula Peyrani, MD Principal Investigator: David Seligson, MD Sub-Investigator: Craig Roberts, MD Principal Investigator: Julio Ramirez, MD Collapse <<

参考文献

[1] Maszkowska J, Białk-Bielińska A, et al. Sorption of sulfisoxazole onto soil--an insight into different influencing factors. Environ Sci Pollut Res Int. 2015 Aug;22(16):12182-9.
[2] Boxwalla M, Matwyshyn G, et al. Involvement of imidazoline and opioid receptors in the enhancement of clonidine-induced analgesia by sulfisoxazole. Can J Physiol Pharmacol. 2010 May;88(5):541-52.
[3] Chan MF, Okun I, Stavros FL, Hwang E, Wolff ME, Balaji VN. Identification of a new class of ETA selective endothelin antagonists by pharmacophore directed screening. Biochem Biophys Res Commun. 1994 May 30;201(1):228-34. doi: 10.1006/bbrc.1994.1693. Erratum in: Biochem Biophys Res Commun 1994 Aug 15;202(3):1744. PMID: 8198578.
[4] Muñoz-Negrete FJ, Pérez-López M, Won Kim HR, Rebolleda G. Nuevos desarrollos en el tratamiento médico del glaucoma [New developments in glaucoma medical treatment]. Arch Soc Esp Oftalmol. 2009 Oct;84(10):491-500. Spanish. doi: 10.4321/s0365-66912009001000003. PMID: 19902393.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.7411 mL
- 18.7053 mL
- 37.4106 mL
- 5 mM
- 0.7482 mL
- 3.7411 mL
- 7.4821 mL
- 10 mM
- 0.3741 mL
- 1.8705 mL
- 3.7411 mL

技术信息

CAS号

127-69-5

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C11H13N3O3S

运输

蓝冰

分子量

267.30

别名

磺胺异恶唑;Sulfafurazole

溶解度

DMSO	110.0 mg/mL (411.5 mM)
Water	insoluble

动物实验配方

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磺胺异噁唑 Catalog No. CSN12014

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