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RS 17053 hydrochloride  ≥98%

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包装规格：1mg 5mg 10mg 25mg in glass bottle
溶解性：溶于DMSO（≥125 mg/mL）
产品描述：基本信息 产品编号： R10311 产品名称： RS 17053 hydrochloride CAS: 169505-93-5   储存条件 粉末 -20℃ 四年     分子式： C24H29ClN2O2.HCl 溶于液体 -80℃ 6个月 分子量： 449.41 -20℃ 1个月 化学名：  (N-[2-(2-CYCLOPROPYLMETHOXYPHENOXY)ETHYL]-5-CHLORO-ALPHA,ALPHA-DIMETHYL-1H-INDOLE-3-ETHANAMINE) HYDROCHLORIDE 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 2.2251mL 11.1257mL 22.2514mL 5mM 0.4450mL 2.2251mL 4.4503mL 10mM 0.2225mL 1.1126mL 2.2251mL   生物活性 产品描述 一种有效的 α1A 肾上腺素受体 (α1A adrenoceptor) 的选择性拮抗剂，其在细胞膜中测得的 pKi 值为 9.1，功能分析的 pA2 值为 9.8。 靶点 pKi:9.1 (α1A adrenoceptor in native cell membrane) pA2:9.8 (α1A adrenoceptor).   体外研究 In several tissues from rat and cloned adrenoceptors,RS 17053 hydrochloride displays high affinity for the α1A-adrenoceptor (pKi and pA2 estimates of 9.1-9.9) and a 30-100-fold selectivity over the α1 B and the α1 D-adrenoceptor subtypes (pKi and pA 2 estimates of 7.7-7.8).However,in isolated smooth muscle preparations from human LUT tissues,RS 17053 hydrochloride antagonizes responses to NE only at high concentrations.Estimates of affinity (pA2) at α1-adrenoceptors mediating NEinduced contractions are 7.5 in prostatic periurethral longitudinal smooth muscle (compared with 8.6 for prazosin),6.9 in anterior fibromuscular stroma (prazosin,8.9),and 7.1 in bladder neck (prazosin,8.5). 体内研究 RS 17053 hydrochloride has a rapid onset of action,and a duration of action exceeding 60 min.RS 17053 hydrochloride pretreatment significantly alteres food intake [F(4,132) 5 6.28,p,0.0001].10mg/kg RS-17053 significantly suppresses food intake.   推荐实验方法(仅供参考) 动物实验:   Rats Adult male rats (n=56 to 8 per group) are pretreated (IP) with either 0,0.1,0.5,2.5,or 10.0mg/kg RS 17053 hydrochloride or with 2.0mg/kg of the prototypical α1-Adrenoceptor antagonist prazosin.Five minutes later, each rat was treated (IP) with either 0,5,10 or 15mg/kg PPA.Food and water intakes are recorded for a 30 min period starting 10 min after the treatment injection.Rats pretreated with vehicle and then treated with PPA exhibite a dose-dependent suppression of feeding with a maximal effect evident at the 15mg/kg dose of PPA.Pretreatment with 2.0mg/kg prazosin reverses the anorexic activity of PPA.
保存条件：-20℃

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