HC-067047 促销  ≥98%

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包装规格:5mg 25mg 50mg in glass bottle
溶解性:溶于DMSO(>15mg/ml)
产品描述:基本信息 产品编号: H10491 产品名称: HC-067047 CAS: 883031-03-6   储存条件 粉末 -20℃ 四年     分子式: C26H28F3N3O2 溶于液体 -80℃ 6个月 分子量: 471.51 -20℃ 1个月 化学名:  2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide Solubility (25°C):   体外:   DMSO 94mg/mL (199.35mM) Ethanol 5mg/mL (10.6mM) 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 2.1208mL 10.6042mL 21.2085mL 5mM 0.4242mL 2.1208mL 4.2417mL 10mM 0.2121mL 1.0604mL 2.1208mL   生物活性 产品描述 一种有效的选择性TRPV4拮抗剂,可逆地抑制流经人,大鼠和小鼠TRPV4直系同源物的电流,IC50值分别为48nM,133nM和17nM。 靶点 IC50:48nM (human TRPV4),133nM (rat TRPV4),17nM (mouse TRPV4)   体外研究 HC-067047 (1µM;24 hours;HEI-OC1 cells) treatment significantly decreases mRNA expression in high glucose cultured HEIOC1 cells.HC-067047 (1µM;24 hours;HEI-OC1 cells) treatment significantly decreases the expression of TRPV4 protein.HC-067047 (1µM;48 hours;HEI-OC1 cells) treatment inhibits cell proliferation.HC-067047 (1µM;48 hours;HEI-OC1 cells) treatment promotes cell apoptosis. RT-PCR Cell Line: HEI-OC1 cells Concentration: 1µM Incubation Time: 24 hours Result: The mRNA expression was significantly decreased. Western Blot Analysis Cell Line: HEI-OC1 cells Concentration: 1µM Incubation Time: 24 hours Result: The expression of TRPV4 protein was significantly decreased. Cell Proliferation Assay Cell Line: HEI-OC1 cells Concentration: 1µM Incubation Time: 48 hours Result: Inhibited cell proliferation. Apoptosis Analysis Cell Line: HEI-OC1 cells Concentration: 1µM Incubation Time: 48 hours Result: Promoted cell apoptosis. 体内研究 HC-067047 (0-50mg/kg;intraperitoneal injection;for 30 minutes;cyclophosphamide-treated WT and Trpv4−/−mice,and naive WT mice) treatment increases functional bladder capacity and reduces micturition frequency in WT mice with cystitis.HC-067047 do not affect bladder function in Trpv4−/−mice. Animal Model: Cyclophosphamide-treated WT and Trpv4−/−mice,and naive WT mice Dosage: 0mg/kg,1mg/kg,10mg/kg,50mg/kg Administration: Intraperitoneal injection;for 30 minutes Result: Increased functional bladder capacity and reduces micturition frequency in WT mice with cystitis and did not affect bladder function in Trpv4−/−mice.
保存条件:-20℃