产品说明书

SC-560

Print
Chemical Structure| 188817-13-2 同义名 : -
CAS号 : 188817-13-2
货号 : A252197
分子式 : C17H12ClF3N2O
纯度 : 99%+
分子量 : 352.738
MDL号 : MFCD02179214
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

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

动物实验配方:
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].
实验方案
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

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.