CAS |
21256-18-8 |
Chinese Name |
奥沙普秦 |
English Name |
Oxaprozin |
Synonyms |
奥沙普秦;4,5-二苯基-2-噁唑丙酸;贝美格;恶丙嗪;3-(4,5-二苯基-1,3-恶唑-2-基)丙酸; |
Molecular Formula |
C18H15NO3 |
Molecular Weight |
293.32 |
Solubility |
Soluble in DMSO ≥5mg/mL |
Purity |
≥98% |
Appearance |
White to off-white Solid |
Storage |
Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC |
EINECS 244-296-1 |
MDL |
MFCD00215977 |
SMILES |
O=C(O)CCC1=NC(C2=CC=CC=C2)=C(C3=CC=CC=C3)O1 |
InChIKey |
OFPXSFXSNFPTHF-UHFFFAOYSA-N |
InChI |
InChI=1S/C18H15NO3/c20-16(21)12-11-15-19-17(13-7-3-1-4-8-13)18(22-15)14-9-5-2-6-10-14/h1-10H,11-12H2,(H,20,21) |
PubChem CID |
4614 |
Target Point |
COX |
Passage |
Immunology & Inflammation |
Background |
It is an inhibitor of COX-1 and COX-2, and also inhibits the activation of NF-κB. |
Biological Activity |
Oxaprozin 是 COX-1 和 COX-2 的抑制剂,对人类血小板 COX-1 和 IL-1 刺激的人类滑膜细胞 COX-2 的 IC50 值分别为 2.2 和 36 μM。Oxaprozin 还能抑制 NF-κB 的活化。[1-2] |
In Vitro |
奥沙普秦以剂量依赖性方式诱导细胞凋亡。奥沙普嗪增加激活但不处于静止状态的胱天蛋白酶-3活性。 50μMOxaprozin抑制NF-κB活化。 Oxaprozin抑制试剂IκBα诱导的IKK系统的激活[1]。奥沙普秦剂量依赖性地增加CD40L处理的单核细胞凋亡。 100μMOxaprozin诱导最强的促凋亡作用。 100μMOxaprozin显著增加CD40L处理的单核细胞凋亡。 Oxaprozin治疗抑制CD40L诱导的Akt和NF-κB(p65)磷酸化[2]。 |
Cell Experiment |
将纯化的单核细胞以106 / mL重悬,并培养48小时。在选择性实验中,在存在或不存在50μMPD98059,1μMSB203580,50μMLY294002,20μMSN-50,50μMAc-DEVD-CHO的情况下培养细胞,不同剂量(5,10,50,100μM))Oxaprozin,100μM布洛芬,100μM吲哚美辛或100μM萘普生。通过荧光显微镜和流式细胞仪测量凋亡细胞的百分比[2]。 |
Kinase Experiment |
在存在或不存在200ng / mL CD40L加1μg/ mL CD40L增强剂和100μM奥沙普秦的情况下进行胱天蛋白酶3活性。假设消光系数为8.8×103M1 / cm [2],在405nm处用分光光度法测定酶活性60分钟。 |
Data Literature Source |
[1]. Ottonello L,et al. Delayed apoptosis of human monocytes exposed to immune complexes is reversed byoxaprozin: role of the Akt/IkappaB kinase/nuclear factor kappaB pathway. Br J Pharmacol. 2009 May;157(2):294-306. [2]. Montecucco F,et al. Oxaprozin-induced apoptosis on CD40 ligand-treated human primary monocytes is associated with the modulation of defined intracellular pathways. J Biomed Biotechnol. 2009;2009:478785. |
Unit |
Bottle |
Specification |
10mg 50mg |