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RO1138452  ≥98%(HPLC)

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO
产品描述：基本信息 产品编号： R10023 产品名称： RO1138452 CAS: 221529-58-4   储存条件 粉末 -20℃ 四年     分子式： C19H23N3O 溶于液体 -80℃ 6个月 分子量： 309.40 -20℃ 1个月 化学名：  4,5-dihydro-N-[4-[[4-(1-methylethoxy)phenyl]methyl]phenyl]-1H-imadazol-2-amine Solubility (25°C)：   体外:   DMSO 62mg/mL (200.38mM) Ethanol 62mg/mL (200.38mM) Water Insoluble 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 3.2320mL 16.1598mL 32.3196mL 5mM 0.6464mL 3.2320mL 6.4639mL 10mM 0.3232mL 1.6160mL 3.2320mL 50mM 0.0646mL 0.3232mL 0.6464mL   生物活性 产品描述 一种IP（prostacyclin）受体拮抗剂，它拮抗氨基前列环素诱导的人神经母细胞瘤腺苷酸环化酶的激活，以剂量依赖的方式阻断环腺苷酸积累。也抑制氚标记的伊洛前列素与啮齿动物神经母细胞瘤细胞的结合，其Ki约为1.5nm。在2-20mg/kg水平的大鼠中，RO1138452在标准抗伤害试验中显示出显著的镇痛活性。 靶点 Prostaglandin Receptor   体外研究 RO1138452 is IP receptor antagonist.The pIC50 values of RO1138452 in attenuating cAMP accumulation is 7.0±0.07.Functional antagonism of RO1138452 is studied by measuring inhibition of carbaprostacyclin-induced cAMP accumulation in CHO-K1 cells stably expressing the human IP receptor.The antagonist affinity (pKi) of RO1138452 is 9.0±0.06. Selectivity profiles for RO1138452 are determined via a panel of receptor binding and enzyme assays.RO1138452 displays affinity at imidazoline2 (I2) (8.3) and platelet activating factor (PAF) (7.9) receptors.RO1138452 (10 pM-10μM) added to cells concurrently with a fixed concentration of Taprostene (1μM) prevents,in a concentration-dependent manner,the inhibition of CXCL9 and CXCL10 release,with p[A]50 (molar) values of -8.73±0.11 and -8.47±0.16 (p>0.05),respectively. 体内研究 RO1138452 is a potent and selective antagonist for both human and rat IP receptors and that is possesses analgesic and antiinflammatory potential.RO1138452 (1-10mg/kg,i.v.) significantly reduces acetic acid-induced abdominal constrictions.RO1138452 (3-100mg/kg,p.o.) significantly reduces carrageenan-induced mechanical hyperalgesia and edema formation.One hour after administration of RO1138452 (5mg/kg,i.v.) to rats, the total plasma concentration is 0.189μg/mL,whereas the free plasma concentrations is calculated to be 0.009μg/mL (28nM).   推荐实验方法(仅供参考) 激酶实验： Selectivity is determined by the ability of RO1138452 (10μM) to displace specific binding of standard radioligands at 51 receptors.When significant displacement of radioligand is observed (>70% for RO1138452),complete concentrationdependent displacement curves (in triplicate) are constructed to generate IC50 values.Displacement binding at the EP3 receptor is performed.Enzyme inhibition assays are also conducted. RO1138452 is evaluated at 10μM in triplicate for inhibition of COX isoforms: COX-1 (ram seminal vesicle),COX-2 (sheep placenta and human umbilical vein). Arachidonic acid is used as a substrate and PGE2 accumulation is detected.   细胞实验:   BEAS-2B cells are incubated for 30 min at 37℃ in supplement-free keratinocyte serum-free medium (KSFM) in the absence and presence of 100nM RO1138452.Cells are washed with supplement-free KSFM,incubated in the same medium for defined periods,and exposed to 1μM Taprostene. Four hours later,cells are harvested in reporter lysis buffer,and luciferase activity is measured.The viability HAECs and BEAS-2B cells is determined colorimetrically by measuring the reduction of the tetrazolium salt MTT to formazan,by mitochondrial dehydrogenases.   动物实验:   Rats Male Sprague-Dawley rats (n=3) are administered RO1138452 (5mg/kg,i.v.).At various times after dose administration,the rats are anesthetized by halothane (5%),blood is collected by orbital bleed into a heparinized syringe and a plasma fraction is obtained by centrifugation of the blood at 2600×g for 5 min in a clinical centrifuge.The level of RO1138452 in each sample is determined by high-performance liquid chromatography with detection by mass spectrometry.
保存条件：-20℃

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