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RS504393  99.66%(HPLC)

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(1mg/mL 加热）
产品描述：基本信息 产品编号： R10038  产品名称： RS504393 CAS: 300816-15-3   储存条件 粉末 -20℃ 四年     分子式： C25H27N3O3 溶于液体 -80℃ 6个月 分子量： 417.50 -20℃ 1个月 化学名：  6-Methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one 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 2.3952mL 11.9760mL 23.9521mL 5mM 0.4790mL 2.3952mL 4.7904mL 10mM 0.2395mL 1.1976mL 2.3952mL   生物活性 产品描述 一种选择性的CCR2拮抗剂,作用于人重组CCR2和CCR1受体，IC50分别为89nM和>100μM。 靶点 CCR   体外研究 RS 504393 inhibits the MCP-1-induced chemotaxis with an IC50 of 330nM.RS 504393 treatment suppresses allergen induced β-hexosaminidase release significantly.Without allergen priming,MCP-1 induces mast cell degranulation,which is completely suppressed by RS 504393. 体内研究 RS504393 (0.3-3μg) with CCL2 progressively blocks thermal hyperalgesia dose-dependently in mice.RS 504393 (5mg/kg,i.v.) supresses the elevated numbers of leukocytes and increased total protein content in BALF induced by The LPS.RS504393 significantly down regulates the LPS-induced elevation of IL-1β,PAI-1 mRNA and protein expressions.RS504393 significantly suppresses induced lung edema, protein-rich fluid, polymorphonuclear accumulation and bronchial wall thickening induced by LPS.RS-504393 significantly reduces renal pathology,especially the extensive interstitial fibrosis mediated by decrease in type I collagen synthesis in a UUO model.   推荐实验方法(仅供参考) 激酶实验： Isolated mast cells are sensitized by incubation with anti-DNP IgE in RPMI1640 containing 10ng/mL of murine recombinant IL-3,10ng/mL of recombinant SCF,and 5% murine serum.The cells are then washed with HBSS containing 10ng/mL of murine recombinant IL-3,10ng/mL of recombinant SCF,0.04% BSA,and 10mM HEPES.Resuspended cells at a concentration of 2 to 8×104 cells/100μL are transferred into triplicate wells of a 96 well U-bottom plate and allowed to equilibrate at 37℃ for 10 minutes before the addition of DNP-albumin or compound 48/80.After 45 minutes,the plate is centrifuged at 290g for 5 minutes at 4℃.The β-hexosaminidase activity of the culture supernatant is determined using a Published protocol.Fifty-μL aliquots of the supernatant are placed in wells of another 96-well plate together with 100 L of 2.5mM p-nitrophenyl-N-acetyl β-d glucosaminide solubilized in 0.04mol/Lcitrate buffer adjusted to pH 4.5 with disodium phosphate.After incubation at 37℃ for 90 minutes,the reactions are terminated by addition of 50μL of 0.4mol/Lglycin adjusted to pH 10.7 with sodium hydroxide.The colored product is measured at 405nm with a reference filter of 570nm.The relative release of β-hexosaminidase is defined as the activity in the supernatant of the tested cells divided by the activity in the positive control cell supernatant,multiplied by 100.Compound 48/80 stimulus is used for assay control.   动物实验:   Male C57BL/6J mice (n=30) and male homozygote CCR1,CCR2 and CCR3 knockout mice (n=12,in each phenotype),6-8 weeks old and weighing 20±2g.Intranasal administration of PBS or LPS (5mg/kg) is performed in a volume of 1mL/kg body weight.C57BL/6J mice are treated with vehicle or RS504393 (5mg/kg) intraperitoneally 30 min before LPS challenge.Four hours after LPS challenge,mice are terminated by an intraperitoneal injection of an overdose of pentobarbitone.The mice are kept on a 12-h light/dark cycle with access to mice chow and water ad libitum.
保存条件：-20℃

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