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trans-ACPD  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(50mg/mL超声）
产品描述：基本信息 产品编号： T70134 产品名称： trans-ACPD CAS: 67684-64-4   储存条件 粉末 -20℃ 四年     分子式： C7H11NO4 溶于液体 -80℃ 6个月 分子量 173.17 -20℃ 1个月 化学名：  1-Amino-cyclopentane-1,3-dicarboxylic acid(trans-(1R,3R)-ACPD) 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 5.7747mL 28.8734mL 57.7467mL 5mM 1.1549mL 5.7747mL 11.5493mL 10mM 0.5775mL 2.8873mL 5.7747mL   生物活性 产品描述 一种代谢型受体激动剂，促进钙离子活动及产生内向电流。 靶点 mGluR   体外研究 Excitatory amino acid (EAA) analogues activate receptors that are coupled to the increased hydrolysis of phosphoinositides (PIs).In these studies,hippocampal slices are prepared from neonatal rats (6-11 days old) to characterize the effects of EAA analogues on these receptors.The concentrations of trans-ACPD required to evoke half-maximal stimulation (EC50 value) is 51μM.DL-2-Amino-3-phosphonopropionate (DL-AP3) is also equipotent as an inhibitor of PI hydrolysis stimulated by ibotenate,quisqualate,and trans-ACPD (IC50 values are 480-850μM). 体内研究 Intrathecal injection of NMDA,kainate,and trans-ACPD,TNF-α,or IL-1β causes significant (p<0.001) biting behaviour in mice compared to animals injected intrathecally with saline.In all groups,systemic pre-treatment with GM (100mg/kg,i.p.) significantly (p<0.001) reduces the biting behaviour compared to mice treated with saline (10mL/kg,i.p.). The greatest effect of GM is observed on the pro-inflammatory cytokines and NMDA,with the following inhibition percentages:TNF-α(92±7%),IL-1β(91±5%),NMDA (69±1%),and trans-ACPD (71±12%).By contrast,at the same dose,GM has no significant effect on the kainate-mediated biting response.   推荐实验方法(仅供参考) 动物实验:   Mice Male Swiss mice (25-35g) are used.Intrathecal injections are given to fully conscious mice.Briefly,the animals are manually restrained,and a 30-gauge needle connected by a polyethylene tube to a 25μL Hamilton gas-tight syringe is inserted through the skin and between the vertebrae into the subdural space of the L5-L6 spinal segments.Intrathecal injections (5μL/site) are administered over a period of 5 s.Biting behaviour is defined as a single head movement directed at the flanks or hind limbs,resulting in contact of the animal's snout with the target organ.The nociceptive response is elicited by NMDA (450 pmol/site,a selective agonist of the NMDA glutamatergic ionotropic receptor),kainate (110 pmol/site,a selective agonist of the kainate subtype of glutamatergic ionotropic receptors),and trans-ACPD (50nmol/site,a non-selective agonist of metabotropic glutamate receptors,which is active at group I and group II),TNF-α(0.1 pmol/site) and IL-1β(1 pmol/site) or saline (5μL/site, i.t.).The amount of time the animal spent biting or licking the caudal region is taken as evidence of nociception and is evaluated following local post injections of the following agonists:NMDA (5 min),kainate (4 min),and trans-ACPD TNF-α,and IL-1β(15 min).Animals received GM (100mg/kg,i.p.) 0.5h before intrathecal injection of 5μL of the drugs,while control animals received a similar volume of saline (10mL/kg, i.p.).
保存条件：-20℃

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