OPC-28326  ≥98%

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产品描述:基本信息 产品编号: O10248  产品名称: OPC-28326 CAS: 167626-17-7   储存条件 粉末 -20℃ 四年 分子式: C26H35N3O2 溶于液体 -80℃ 二年 分子量: 421.58     化学名:  N-[2,6-dimethyl-4-[4-[methyl(2-phenylethyl)amino]piperidine-1-car onyl]phenyl]propanamide 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。   生物活性 产品描述 一种外周血管扩张药,同时为 α2-adrenergic receptor 的拮抗剂,对 α2A-,α2B- 和 α2C 肾上腺素受体的 Ki 值分别为 2040,285 和 55nM。 靶点 Ki:2040nM (α2A adrenoceptor),285nM (α2B adrenoceptor),55nM (α2C adrenoceptor)   体外研究 OPC-28326 enhances endothelial tube formation and promotes microvessel growth. OPC-28326 induces phosphorylation of eNOS and Akt in HAECs in a dose dependent-manner,while it does not affect total amounts of eNOS and Akt.OPC-28326 (1-100μM) and yohimbine (10-1000nM) causes a rightward shift in the concentration-response curve of clonidine. 体内研究 OPC-28326 augments blood flow recovery in murine hindlimb ischemia.OPC-28326 significantly increases the number of histologically detectable capillaries in the ischemic leg.OPC-28326 has no beneficial effects on blood flow recovery in eNOS−/− mice.OPC-28326 (3-30mg/kg,i.v.) and yohimbine causes dose-dependent rightward shift in the pressor doseresponse curve induced by B-HT 920.OPC-28326 does not affect on the mydriasis in rats.   推荐实验方法(仅供参考) 动物实验:   Unilateral hindlimb ischemia is induced in 30-to 35-week-old male mice by resecting the right femoral and saphenous arteries.The mice are fed on regular chow (Ctrl),chow containing 0.02% (OPC(L)) or 0.05% (OPC(H)) OPC-28326,starting one week before the surgery (n=10 for each group).Hindlimb blood perfusion is measured using a laser Doppler perfusion imager (LDPI) system.Excess hairs are removed from the limbs using depilatory cream before imaging,and mice are placed on a heating plate at 40℃.To avoid the influence of ambient light and temperature,the results are expressed as the ratio of perfusion in the right (ischemic) versus left (untreated) limb.The thigh muscles are harvested at 4 weeks and stained for CD31 (clone MEC13.1) to detect endothelial cells.Capillaries are identified by positive staining for CD31 and their morphology.Ten different fields from each tissue preparation are randomly selected and capillaries are counted.Capillary density is expressed as the number of capillaries per square millimeter.
保存条件:-20℃