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SC-560 {[allProObj[0].p_purity_real_show]}

货号:A252197

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。

SC-560 化学结构 CAS号:188817-13-2
SC-560 化学结构
CAS号:188817-13-2
SC-560 3D分子结构
CAS号:188817-13-2
SC-560 化学结构 CAS号:188817-13-2
SC-560 3D分子结构 CAS号:188817-13-2
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SC-560 纯度/质量文件 产品仅供科研

货号:A252197 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

SC-560 生物活性

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].

SC-560 参考文献

[1]Paskauskas S, Parseliunas A, et al. Blockade of leukocyte haptokinesis and haptotaxis by ketoprofen, diclofenac and SC-560. BMC Immunol. 2011 Nov 12;12:64.

[2]Teng XW, Abu-Mellal AK, Davies NM. Formulation dependent pharmacokinetics, bioavailability and renal toxicity of a selective cyclooxygenase-1 inhibitor SC-560 in the rat. J Pharm Pharm Sci. 2003 May-Aug;6(2):205-10.

[3]Smith CJ, Zhang Y, Koboldt CM, Muhammad J, Zweifel BS, Shaffer A, Talley JJ, Masferrer JL, Seibert K, Isakson PC. Pharmacological analysis of cyclooxygenase-1 in inflammation. Proc Natl Acad Sci U S A. 1998 Oct 27;95(22):13313-8. doi: 10.1073/pnas.95.22.13313. PMID: 9789085; PMCID: PMC23795.

[4]Brenneis C, Maier TJ, Schmidt R, Hofacker A, Zulauf L, Jakobsson PJ, Scholich K, Geisslinger G. Inhibition of prostaglandin E2 synthesis by SC-560 is independent of cyclooxygenase 1 inhibition. FASEB J. 2006 Jul;20(9):1352-60. doi: 10.1096/fj.05-5346com. PMID: 16816110.

SC-560 实验方案

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

SC-560 技术信息

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

请根据您的动物给药指南选择适当的溶解方案。
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
方案一
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