产品说明书
Sulfisoxazole
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同义名 : | 磺胺二甲异唑 ;Sulfafurazole;NSC 13120;Neoxazol;Neazolin;NSC 683536;NSC 38588;NSC 33807;NU-445 |
| CAS号 : | 127-69-5 | |
| 货号 : | A450666 | |
| 分子式 : | C11H13N3O3S | |
| 纯度 : | 97% | |
| 分子量 : | 267.304 | |
| MDL号 : | MFCD00003150 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 145 mg/mL(542.45 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 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]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| 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 ... 展开 >> 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 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.74mL 0.75mL 0.37mL |
18.71mL 3.74mL 1.87mL |
37.41mL 7.48mL 3.74mL |
| 参考文献 |
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