SC-560是一种高度选择性的环氧合酶-1(COX-1)抑制剂(COX-1和COX-2的IC50分别为0.009 μM和6.3 μM)。它抑制COX-1衍生的血小板血栓素B2、胃PGE2和皮肤PDE2的生成,并显著减少体内卵巢表面上皮肿瘤的生长。
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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 |
95% | |||||||||||||||||
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 |
99% | ||||||||||||||||
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。 |
描述 | The cyclooxygenase (COX) enzymes (COX-1 and COX-2) catalyze the bis-oxygenation of free arachidonic acid to prostaglandin (PG) H2, the precursor of other PGs and thromboxane (Tx). SC-560 is a selective COX-1 inhibitor with an IC50 value of 9 nM. It shows much less inhibitory potency against COX-2 with an IC50 value of 6.3 μM[3]. SC-560 decreased COX-1-dependent TxB2 production in human platelets with an IC50 value of 2.5 nM. It also reduced COX-2-dependent PGE2 synthesis in LPS-stimulated human monocytes with an IC50 value of 1.8 nM[4]. Oral administration of SC-560 (10 or 30 mg/kg) one hour before the whole blood assay inhibited ionophore-stimulated TxB2 production in rats. Oral dosing with SC-560 (0.1-100 mg/kg) blocked the production of TxB2 in a concentration-dependent manner in rat inflamed skin. SC-560 at 100 mg/kg showed 40% inhibition on PGE2 production in LPS-induced rat air pouch. It also efficiently inhibited PGE2 synthesis in stomach mucosa with an ED50 value of 0.2 mg/kg. However, 30 mg/kg SC-560 exhibited no significant effect on the onset of edema or hyperalgesia[3]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.83mL 0.57mL 0.28mL |
14.17mL 2.83mL 1.42mL |
28.35mL 5.67mL 2.83mL |
CAS号 | 188817-13-2 |
分子式 | C17H12ClF3N2O |
分子量 | 352.74 |
SMILES Code | FC(C1=NN(C2=CC=C(OC)C=C2)C(C3=CC=C(Cl)C=C3)=C1)(F)F |
MDL No. | MFCD02179214 |
别名 | |
运输 | 蓝冰 |
InChI Key | PQUGCKBLVKJMNT-UHFFFAOYSA-N |
Pubchem ID | 4306515 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, 2-8°C |
溶解方案 |
DMSO: 105 mg/mL(297.67 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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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