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CAS No.: 188817-13-2

SC-560 Catalog No. CSN20354

Synonyms: SC-560

SC-560 is a highly selective cyclooxygenase-1 (COX-1) inhibitor (IC50 values are 0.009 and 6.3 μM for COX-1 and COX-2 respectively). It inhibits COX-1-derived platelet thromboxane B2, gastric PGE2 and dermal PDE2 production and significantly reduces ovarian surface epithelial tumor growth in vivo.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 COX1

IC50:0.009μM COX2

IC50:6.3μM
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].
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8350 mL
- 14.1748 mL
- 28.3496 mL
- 5 mM
- 0.5670 mL
- 2.8350 mL
- 5.6699 mL
- 10 mM
- 0.2835 mL
- 1.4175 mL
- 2.8350 mL

技术信息

CAS号

188817-13-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H12ClF3N2O

运输

蓝冰

分子量

352.74

别名

SC-560

溶解度

DMSO	190.0 mg/mL (538.6 mM)
Water	insoluble

动物实验配方

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靶点	Description	IC50
COX1		IC50:0.009μM
COX2		IC50:6.3μM

SC-560 Catalog No. CSN20354

靶点选择性

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