货号:A395168 同义名: Oxaprozinum;Wy21743
Oxaprozin is a COX inhibitor with IC50s of 2.2 μM and 36 μM for human platelet COX-1 and IL-1-stimulated human synovial cell COX-2, it's a NSAID used to relieve the inflammation, swelling, stiffness, and joint pain associated with osteoarthritis and rheumatoid arthritis.
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产品名称 | COX ↓ ↑ | COX-1 ↓ ↑ | COX-2 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Piroxicam | ✔ | 98% | |||||||||||||||||
Salicylic acid | ✔ | 98% | |||||||||||||||||
Phenacetin | ✔ | 98% | |||||||||||||||||
Etodolac | ✔ | 99% | |||||||||||||||||
Flunixin meglumine | ✔ | 98% | |||||||||||||||||
Ibuprofen L-lysine | ✔ | 99% | |||||||||||||||||
Nabumetone | ✔ | 98% | |||||||||||||||||
Acemetacin | ✔ | 98% | |||||||||||||||||
Diflunisal | ✔ | 98% | |||||||||||||||||
Pranoprofen | ✔ | 98% | |||||||||||||||||
Ampiroxicam | ✔ | 98% | |||||||||||||||||
Meloxicam | ✔ | 98% | |||||||||||||||||
Sulindac | ✔ | 98% | |||||||||||||||||
Ketoprofen | ✔ | 98% | |||||||||||||||||
Mefenamic Acid | ✔ | 95% | |||||||||||||||||
Bromfenac sodium | ✔ | 98% | |||||||||||||||||
Oxaprozin | ✔ | 99% | |||||||||||||||||
Aspirin | ✔ | 99% | |||||||||||||||||
Nepafenac | ✔ | 98% | |||||||||||||||||
Zaltoprofen | ✔ | 99% | |||||||||||||||||
Salicin | ✔ | 98% | |||||||||||||||||
Suprofen | ✔ | 99%+ | |||||||||||||||||
Xanthohumol | ✔ | 99% | |||||||||||||||||
Parecoxib | ✔ | 98% | |||||||||||||||||
Tolfenamic Acid |
+++
COX-2, IC50: 0.2 μM |
98% | |||||||||||||||||
Etoricoxib | ✔ | 99% | |||||||||||||||||
Niflumic Acid | ✔ | 98% | |||||||||||||||||
Valdecoxib |
++++
COX-2, IC50: 5 nM |
99+% | |||||||||||||||||
Ibuprofen |
+
COX-1, IC50: 13 μM |
+
COX-2, IC50: 370 μM |
98% | ||||||||||||||||
Indomethacin |
++
COX1, IC50: 0.28 μM |
+
COX-2, IC50: 14 μM |
97% | ||||||||||||||||
Lornoxicam |
++++
COX-1, IC50: 5 nM |
++++
COX-2, IC50: 8 nM |
98% | ||||||||||||||||
Meclofenamic acid sodium |
++++
COX-1, IC50: 40 nM |
+++
COX-2, IC50: 50 nM |
99% | ||||||||||||||||
Rofecoxib |
++++
COX-2, IC50: 18 nM |
98% | |||||||||||||||||
Asaraldehyde | ✔ | 98% | |||||||||||||||||
Naproxen |
+
COX-1, IC50: 8.7 μM |
+
COX-2, IC50: 5.2 μM |
98% | ||||||||||||||||
Diclofenac Sodium Salt |
+++
COX-1, IC50: 60 nM |
+++
COX-2, IC50: 200 nM |
98% | ||||||||||||||||
NS-398 |
++
COX-2, IC50: 3.8 μM |
98% | |||||||||||||||||
Amfenac Sodium Hydrate |
++
COX-1, IC50: 250 nM |
+++
COX-2, IC50: 150 nM |
98%+ | ||||||||||||||||
Nimesulide |
+
COX-2, IC50: 26 μM |
98% | |||||||||||||||||
Lumiracoxib |
++
COX-1, Ki: 3 μM |
+++
COX-2, Ki: 60 nM |
98% | ||||||||||||||||
Rutaecarpine | ✔ | 95% | |||||||||||||||||
Celecoxib |
++++
COX-2, IC50: 40 nM |
98% | |||||||||||||||||
Carprofen |
++++
canine COX2, IC50: 30 nM |
98% | |||||||||||||||||
Ketorolac |
++
COX-1 (human), IC50: 1.23 μM |
++
COX-2 (human), IC50: 3.50 μM |
98% | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Oxaprozin is an inhibitor of both COX-1 and COX-2 with IC50s of 2.2 μM and 36 μM for human platelet COX-1 and IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB. Oxaprozin reversed in a dose-dependent manner immune complex-induced survival of monocytes, without affecting the apoptosis of resting cells. Other NSAIDs (Non-steroidal anti-inflammatory drugs) are ineffective. Oxaprozin-mediated inhibition of the Akt/IKK/NF-kappaB pathway contributes to its anti-inflammatory properties[3]. Among different NSAIDs, only oxaprozin dose-dependently increased apoptosis of CD40L-treated monocytes. Oxaprozin pro-apoptotic activity was associated with the inhibition of CD40L-triggered Akt and NF-kappaB phosphorylation and the activation of caspase 3[4]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT03350386 | Healthy | Phase 1 | Completed | - | Japan ... 展开 >> P-One Clinic Hachiōji, Tokyo, Japan, 192-0071 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.41mL 0.68mL 0.34mL |
17.05mL 3.41mL 1.70mL |
34.09mL 6.82mL 3.41mL |
CAS号 | 21256-18-8 |
分子式 | C18H15NO3 |
分子量 | 293.317 |
别名 | Oxaprozinum;Wy21743;Oxaprozin, Oxaprozinum, DL-8280, DR-3355, Hoe-280, ORF-28489, Ru-43280, Tarivid;NSC 310839 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Room Temperature |
溶解度 |
DMSO: 105 mg/mL(357.97 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 |
动物实验配方 |