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SC-560
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SC-560图片
CAS NO:188817-13-2
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
SC560
产品介绍
SC560 是一种选择性COX-1抑制剂,IC50值为 9 nM。

产品描述

SC-560 is a member of the diaryl heterocycle class of cyclooxygenase (COX) inhibitors.

体外活性

Preincubation of COX-1 with SC-560 inhibits the conversion of arachidonic acid to PGE2 in a concentration-dependent manner. The IC50 of SC-560 for COX-2 is 6.3 μM, nearly 1,000-fold higher than with COX-1. SC-560 exhibits a dose and time-dependent inhibitory effect on HCC cell growth. SC-560 also inhibits colony formation in soft agar and induces apoptosis in HCC cells in a dose-dependent manner. Moreover, SC-560 decreases the levels of the anti-apoptotic proteins survivin and XIAP and activates caspase 3 and 7 in a dose and time-dependent fashion.

体内活性

Oral dosing with either 10 or 30 mg/kg SC-560 1 hour before assay completely inhibits ionophore-stimulated TxB2production, indicating that SC-560 is orally bioavailable and inhibits COX-1 in vivo. SC-560 extensively distributes into rat tissues, and has a CL approaching hepatic plasma flow. After oral administration, the drug exhibits low less than 15% formulation-dependent bioavailability and demonstrates kidney toxicity.

激酶实验

Test compound is incubated with human whole blood stimulated with bacterial LPS for 4 h, followed by capture of MPO on immobilized anti-MPO antibody coated plates. The captured MPO is washed and residual MPO activity is determined using Amplex Red and H2O2.

细胞实验

SC-560 is dissolved in DMSO[2].HuH-6 and HA22T/VGH cells (5000/well) are treated with various concentrations of SC-560 (5, 10, 25, 50, 100, 200 μM) and cultured for 72 h. At the end of treatment, cell viability is assessed by MTS assay.

动物实验

Rat: The pharmacokinetics of SC-560 is studied in Sprague-Dawley rats after a single intravenous (i.v.) and oral dose (10 mg/kg) in polyethylene glycol (PEG) 600 and a single oral dose (10 mg/kg) in 1% methylcellulose (MC). Serial blood samples are collected via a catheter inserted in the right jugular vein and serum samples are analysed for SC-560 using reverse phase HPLC. After oral administration of SC-560 in PEG, urine is also collected for 24 h and analyzed for urinary sodium, chloride, and potassium as well as NAG.

Cas No.

188817-13-2

分子式

C17H12ClF3N2O

分子量

352.74

别名

SC560

储存和溶解度

DMSO:35.3 mg/mL(100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years