INCB 3284  ≥98%

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包装规格:1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性:溶于DMSO(≥ 83.3 mg/mL)
产品描述:基本信息 产品编号: I10605 产品名称: INCB 3284 CAS: 887401-92-5   储存条件 粉末 -20℃ 四年     分子式: C26H31F3N4O4 溶于液体 -80℃ 6个月 分子量: 520.54 -20℃ 1个月 化学名:  N-[2-[[(3R)-1-[4-hydroxy-4-(6-methoxypyridin-3-yl)cyclohexyl]pyrrolidin-3-yl]amino]-2-oxoethyl]-3-(trifluoromethyl)benzamide 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 1.9211mL 9.6054mL 19.2108mL 5mM 0.3842mL 1.9211mL 3.8422mL 10mM 0.1921mL 0.9605mL 1.9211mL   生物活性 产品描述 一种有效的,选择性的人 CCR2 拮抗剂,能够抑制单核细胞趋化蛋白 1 与 hCCR2 结合,IC50 值为 3.7nM。INCB 3284 可用于急性肝功能衰竭的研究。 靶点 MCP-1-hCCR2 3.7nM (IC50)   体外研究 INCB 3284 is a pentent,selective and orally bioavailable human CCR2 antagonist,inhibiting monocyte chemoattractant protein-1 binding to hCCR2,with an IC50 of 3.7nM.INCB 3284 also causes an IC50 of 4.7nM in antagonism of chemotaxis activity,an IC50 of 84μM in inhibition of the hERG potassium current.However,INCB 3284 has no effec on CCR1,CCR3,CCR5,CXCR3,and CXCR5,or additional GPCRs at a concentration of 1μM.Moreover,INCB 3284 potently inhibits CCR2-mediated signaling events such as intracellular calcium mobilization and ERK phosphorylation with IC50 values of 6 and 2.6nM,respectively. 体内研究 INCB 3284 (1mg/kg/day,ip) reduces liver damage,and decreases microglia activation in AOM-treated mice via inhibition on CCR2.INCB 3284 also significantly reduces the pERK1/2 to tERK1/2 ratio,as well as G-protein signaling pathway activity and proinflammatory cytokine production in cortex lysates from mice administed with azoxymethane.   推荐实验方法(仅供参考) 动物实验:   Mice Male C57Bl/6 mice (20 to 25g) are given free access to water and rodent chow and are housed in constant temperature,humidity,and 12h light-dark cycling.Acute liver failure is induced via a single intraperitoneal (ip) injection of 100mg/kg of azoxymethane (AOM).In parallel,systemic inhibition of CCR2 and CCR4 activity is accomplished via pretreatment with INCB 3284 (1mg/kg/day ip) or C021 (1mg/kg/day ip) for 3 days prior to injection of AOM.Following injection,mice are placed on heating pads adjusted to 37℃ and monitored frequently for signs of neurological decline.To reduce the impacts of hypoglycemia and dehydration,cage floors are supplied with hydrogel and rodent chow and after 12h,and every subsequent 4h,mice are injected subcutaneously with 5% dextrose in 250μL of saline.If mice undergo a 20% or greater weight loss they are removed from the study.
保存条件:-20℃