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Sulfasalazine

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Chemical Structure| 599-79-1 同义名 : 柳氮磺胺吡啶 ;NSC 667219;Azopyrin;Rorasul;Reupirin;NSC-203730 NSC 203730;NSC 203730;Sulphasalazine
CAS号 : 599-79-1
货号 : A176325
分子式 : C18H14N4O5S
纯度 : 98%
分子量 : 398.39
MDL号 : MFCD00057363
存储条件:

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 85 mg/mL(213.36 mM),配合低频超声,并水浴加热至45℃助溶,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

NH4OH: 150 mg/mL(376.52 mM),配合低频超声,并调节pH至9

动物实验配方:
生物活性
描述 Sulfasalazine is a potent and specific inhibitor of NF-kappaB activation. Treatment of SW620 colon cells with sulfasalazine inhibited TNFalpha-, LPS-, or phorbol ester- induced NF-kappaB activation. NF-kappaB-dependent transcription was inhibited by sulfasalazine at micro- to millimolar concentrations. TNFalpha-induced nuclear translocation of NF-kappaB was prevented by sulfasalazine through inhibition of IkappaBalpha degradation[3]. Sulfasalazine is a direct inhibitor of IKK-alpha and -beta by antagonizing adenosine triphosphate binding. The suppression of NF-kappaB activation by inhibition of the IKKs contributes to the well-known anti-inflammatory and immunosuppressive effects of sulfasalazine[4]. Sulfasalazine can inhibit NF-κB and reduce lipopolysaccharide-induced cytokine concentrations in fetal membrane explants and reduce the rate of Escherichia coli-induced preterm labour in mice[5]. Sulfasalazine induces cell death via apoptosis in HBx-expressing liver cells, as evidenced by characteristic changes in nuclear morphology, cleavage of poly (ADP-ribose) polymerase (PARP), caspase-3 and caspase-9, and activation of caspase-3[6].
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
NCT02930343 Rheumatoid Arthritis Phase 4 Recruiting August 2018 India ... 展开 >> Department of Clinical Immunology , Jawaharlal Institute of Post graduate Medical Educationa and Research Recruiting Pondicherry, India, 605006 Contact: Dr. Vir Singh Negi, DM    0413-2297358    vsnegi22@yahoo.co.in    Contact: Dr. Pooja Belani, MD    8940482248    drpoojabelani@gmail.com 收起 <<
NCT02590562 - Completed - China ... 展开 >> Peking University First Hospital Beijing, China, 100034 Beijing Jishutan Hospital; Rheumatology & Immunology Beijing, China, 100035 Peking University People's Hospital Beijing, China, 100044 Peking University Third Hospital Beijing, China, 100083 China-Janpan Friendship Hospital of Jilin University Changchun, China, 130031 West China Hospital, Sichuan University Chengdu, China, 610041 Sichuan Provincial People's Hospital Chengdu, China, 610072 The First Affiliated Hospital, Sun Yat-sen University Guangzhou, China, 510080 The First Affiliated Hospital of Guangzhou University of Chinese Medicine Guangzhou, China, 510405 Nanfang Hospital, Southern Medical University Guangzhou, China, 510515 Guanghua Hospital of Integrated Traditional Chinese and Western Medicine ( Guanghua Hospital) Shanghai, China, 200052 The Second Hospital of Shanxi Medical University Taiyuan, China, 030001 Tianjin Medical University General Hospital Tianjin (天津), China, 300052 First Affiliated Hospital of Medical College of Xi'an Jiaotong University Xi'an, China, 710061 Xinjiang Uygur Autonomous Region People Hospital Ürümqi, China, 830001 收起 <<
NCT02590562 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.51mL

0.50mL

0.25mL

12.55mL

2.51mL

1.26mL

25.10mL

5.02mL

2.51mL

参考文献

[1]Liptay S, Bachem M, et al. Inhibition of nuclear factor kappa B and induction of apoptosis in T-lymphocytes by sulfasalazine. Br J Pharmacol. 1999 Dec;128(7):1361-9.

[2]Gadangi P, Longaker M, et al. The anti-inflammatory mechanism of sulfasalazine is related to adenosine release at inflamed sites. J Immunol. 1996 Mar 1;156(5):1937-41.

[3]Wahl C, Liptay S, Adler G, Schmid RM. Sulfasalazine: a potent and specific inhibitor of nuclear factor kappa B. J Clin Invest. 1998 Mar 1;101(5):1163-74

[4]Weber CK, Liptay S, Wirth T, Adler G, Schmid RM. Suppression of NF-kappaB activity by sulfasalazine is mediated by direct inhibition of IkappaB kinases alpha and beta. Gastroenterology. 2000 Nov;119(5):1209-18

[5]Sykes L, Thomson KR, Boyce EJ, Lee YS, Rasheed ZB, MacIntyre DA, Teoh TG, Bennett PR. Sulfasalazine augments a pro-inflammatory response in interleukin-1β-stimulated amniocytes and myocytes. Immunology. 2015 Dec;146(4):630-44

[6]Lee YM, Kang M, Hwang JM, Lee S, Cho H, Kim YS. Sulfasalazine induces apoptosis of HBx-expressing cells in an NF-kappaB-independent manner. Virus Genes. 2010 Feb;40(1):37-43