中文名称: | DuP 734 | ||||
---|---|---|---|---|---|
英文名称: | DuP 734 | ||||
别名: | 1-(Cyclopropylmethyl)-4-(2'-(4''-fluorophenyl)-2'-oxoethyl)piperidine | ||||
CAS No: | 135135-87-4 | 分子式: | C17H23BrFNO | 分子量: | 356.27 |
CAS No: | 135135-87-4 | ||||
分子式: | C17H23BrFNO | ||||
分子量: | 356.27 |
基本信息
产品编号: |
D11523 |
||||
产品名称: |
DuP 734 |
||||
CAS: |
135135-87-4 |
储存条件 |
粉末 |
-20℃ |
四年 |
分子式: |
溶于液体 |
-80℃(存于氮气,防潮) |
6个月 |
||
分子量: |
356.27 |
-20℃(存于氮气,防潮) |
1个月 |
||
化学名: |
1-(Cyclopropylmethyl)-4-(2'-(4''-fluorophenyl)-2'-oxoethyl)piperidine |
||||
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 |
2.8069mL |
14.0343mL |
28.0686mL |
5mM |
0.5614mL |
2.8069mL |
5.6137mL |
10mM |
0.2807mL |
1.4034mL |
2.8069mL |
生物活性
产品描述 |
一种 sigma 受体拮抗剂,DuP 734 是一种有效的选择性 sigma 和 5-HT2 受体配体,对 D2 受体的亲和力弱。DuP 734 具有抗精神病活性,而没有抗精神病剂常见的副作用。 |
靶点 |
Sigma receptor;5-HT2 receptor;D2 receptor |
体内研究 |
DuP 734 potently blocks mescaline-induced scratching (ED50=0.35mg/kg,p.o.) and aggressive activity (ED50=1.9mg/kg,p.o.) and is relatively much weaker as an apomorphine antagonist (ED50=12mg/kg,p.o.).Administration of DuP 734 potently antagonizes the binding of [3H]DuP 734 and [3H](+)-SKF 10,047 to brain sigma receptors in vivo with ID50 values of 0.02 and 0.07mg/kg (0.07 and 0.25μmol/kg),respectively.Following intravenous dosing,the disposition of DuP 734 in mice,rats,beagle dogs and cynomolgus monkeys is characterized by high total body systemic plasma clearance (46 to 87mL/min/kg) and large steady-state volume of distribution (3.6 to 6.8L/kg).The terminal elimination half-life ranged from 50 to 83 min.The gastrointestinal absorption from an aqueous solution is very rapid in mice and rats with peak DuP 734 plasma concentrations attain within 5 and 20 min following administration,respectively.The peak plasma concentrations in dogs and monkeys are attained within 45 and 130 min,respectively.The absolute bioavailability in mice ranges from 29 to 46% at doses of 3.1 to 30.1mg/kg.The bioavailability increases from 4 to 10% and from 14 to 72% when doses are increased from 12.5 to 50mg/kg and 1 to 3mg/kg of DuP 734 in rats and dogs, respectively.The bioavailability in monkeys is 30.5% at 9.3mg/kg DuP 734 dose.The dose dependent pharmacokinetics of DuP 734 is observed within narrow dose ranges in all animal species investigated. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )