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RS102895  ≥98%(HPLC)

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包装规格：5mg 25mg 100mg in glass bottle
产品描述：基本信息 产品编号： R10041  产品名称： RS102895 HCl CAS: 300815-41-2   储存条件 粉末 -20℃ 四年     分子式： C21H22ClF3N2O2 溶于液体 -80℃ 6个月 分子量： 426.86 -20℃ 1个月 化学名：  1'-[2-[4-(Trifluoromethyl)phenyl]ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one hydrochloride Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.3427mL 11.7134mL 23.4269mL 5mM 0.4685mL 2.3427mL 4.6854mL 10mM 0.2343mL 1.1713mL 2.3427mL   生物活性 产品描述 一种有效的CCR2 拮抗剂。 靶点 CCR   体外研究 RS102895 hydrochloride is a potent CCR2 antagonist, with an IC50 of 360nM,and shows no effect on CCR1.RS102895 also inhibits human α1a and α1d receptors,rat brain cortex 5HT1a receptor in cells with IC50s of 130,320,470nM,respectively.RS102895 suppresses wild type and D284N mutant MCP-1 receptor (IC50,550nM and 568nM,respectively),less potently inhibits D284A MCP-1 receptor (IC50,1892nM),and has no effects on E291A,E291Q,D284A/E291A or D284N/E291Q (IC50,>100,000nM).RS102895 ameliorates the increased extracellular matrix (ECM) protein expression by inhibition of CCR2 at 10μM,and obviously blocks fibronectin and type IV collagen protein expression in high glucose (HG)-stimulated mesangial cells (MCs) at 1 or 10μM.RS102895 (10μM) also abrogates the increased TGF-1 levels in MCs treated with MCP-1. 体内研究 RS102895 (3g/L) causes progressive decrease in pain threshold in rats with bone cancer pain (BCP) at day 3-9 after surgery via intrathecal injection,but the pain threshold increases after 12 days.RS102895 also potently reverses the pattern of NR2B,nNOS,and SIGIRR expression in spinal cord.   推荐实验方法(仅供参考) 细胞实验:   Transfected mesangial cells (MCs) are serum restricted for 24h,after which the medium is replaced by serum-free DMEM containing normal glucose (NG;5.6mM),NG+Mannitol (NG+M;24.4mM),or high glucose (HG;30mM).In addition,nontransfected MCs are cultured under NG,NG+M,or HG with or without RS102895 or anti-TGF-1 antibody (25μg/mL).Nontransfected MCs are also exposed to medium containing recombinant human MCP-1 (10ng/mL) or recombinant human TGF-1 (2ng/mL).At 24h after the media change,cells are harvested and the conditioned culture media are collected.   动物实验:   Rats CCR2 antagonist RS102895 is dissolved in DMSO.Rats receive daily intrathecal injection of either RS102895 (3g/L) 10μL or 10 % DMSO 10μL between 9 and 20 days after operation.All rats are randomLy divided into five groups (n=10 per group):Sham group, Sham+RS102895 group,BCP group,BCP+RS102895 group,and BCP+DMSO group.Rats are sacrificed 20 days after operation and the tissue samples from the L4-L5 spinal cord segments are rapidly removed and immediately frozen in liquid nitrogen and stored at −80℃ until use for RT-PCR and Western blot.
保存条件：-20℃

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