SC-560 (188817-13-2) is a highly selective (700-fold selective over COX-2) and potent (IC50 = 9 nM) inhibitor of cyclooxygenase-1(COX-1).1 SC-560 inhibited TNF α-induced PGE2 synthesis in neurons and, PGE2 and thromboxane A2 synthesis in human monocytes and platelets (IC50’s = 1.8 nM and 2.5 nM respectively) indicating non-selective COX inhibition. SC-560 was able to inhibit PGE2 synthesis in COX-1-deficient neurons indicating a COX-1 independent mechanism. This unselective COX inhibition was only observed in whole cells – it remained COX-1 specific in cell lysates.2 选择性COX-1抑制剂sc -560(188817-13-2)是环氧合酶-1(COX-1)的高选择性(选择性是COX-2的700倍)和强效(IC50 = 9 nM)抑制剂 SC-560抑制了TNF α诱导的神经元中PGE2的合成,抑制了人单核细胞和血小板中PGE2和血栓素A2的合成(IC50分别为1.8 nM和2.5 nM),表明非选择性COX抑制。 SC-560能够抑制COX-1缺失神经元中PGE2的合成,表明这是一种不依赖于COX-1的机制。 这种非选择性的COX抑制只在整个细胞中观察到,它在细胞裂解物中仍然具有COX-1特异性。
References/Citations:
1) Smith et al. (1998), Pharmacological analysis of cyclooxygenase-1 in inflammation; Proc. Natl. Acad. Sci. USA 95 13313 2) Brenneis et al. (2006), Inhibition of prostaglandin E2 synthesis by SC-560 is independent of cyclooxygenase 1 inhibition; FASEB J. 20 1352
CAS:
18817-13-2
Catalog Number:
10-2531
Activity:
Selective COX-1 inhibitor
Chemical Name:
5-(4-Chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazole
Molecular Weight:
352.74
Molecular Formula:
C17H12ClF3N2O
Solubility:
Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to 10 mg/ml)
Physical Properties:
Brown solid
Purity:
98%
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT
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