2-Phenyl-2-(1-piperidinyl)propane
(Synonyms: 1-(1-甲基-1-苯基乙基)哌啶) 目录号 : GC12262
A selective inhibitor of CYP2B6
Cas No.:92321-29-4
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
KI: 11 microM for 7-(benzyloxy)resorufin O-dealkylation activity of liver microsomes obtained from phenobarbital-induced rats
2-Phenyl-2-(1-piperidinyl)propane is a mechanism-based inactivator of human cytochrome P450 (CYP) 2B6.
The use of selective chemical inhibitors of human cytochrome P450 enzymes is a powerful method by which the relative contributions of different human P450 enzymes to the drug metabolism can be obtained. However, the contribution of CYP2B6 in the metabolism is more challenging due to the lack of a well-established inhibitor.
In vitro: Previous study found that 2-phenyl-2-(1-piperidinyl)propane could inactivate the 7-(benzyloxy)resorufin O-dealkylation activity of liver microsomes obtained from phenobarbital-induced rats. The 7-ethoxy-4-(trifluoromethyl)coumarin O-deethylation activity of purified rat liver P450 2B1 and expressed human P450 2B6 was also inactivated by 2-phenyl-2-(1-piperidinyl)propane in a reconstituted system. With NADPH, the loss of activity was founf to be both time- and concentration-dependent, and followed pseudo first order kinetics. The time for 50% of the P450 2B1 to become inactivated at saturating concentrations of 2-phenyl-2-(1-piperidinyl)propane was ~2.5 min. P450 2B6 was inactivated by 2-phenyl-2-(1-piperidinyl)propane with a k(inact) of 0.07 min(-1), a K(I) of 1.2 microM, and a t(1/2) of 9.5 min. The inactivated P450s 2B1 and 2B6 lost about 25 and 15%, respectively, indicating that the loss of activity was caused by a 2-phenyl-2-(1-piperidinyl)propane modification of the apoprotein rather than the heme [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Chun J, Kent UM, Moss RM, Sayre LM, Hollenberg PF. Mechanism-based inactivation of cytochromes P450 2B1 and P450 2B6 by 2-phenyl-2-(1-piperidinyl)propane. Drug Metab Dispos. 2000 Aug;28(8):905-11.
| Cas No. | 92321-29-4 | SDF | |
| 别名 | 1-(1-甲基-1-苯基乙基)哌啶 | ||
| 化学名 | 1-(1-methyl-1-phenylethyl)-piperidine | ||
| Canonical SMILES | CC(C1=CC=CC=C1)(C)N2CCCCC2 | ||
| 分子式 | C14H21N | 分子量 | 203.3 |
| 溶解度 | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 4.9188 mL | 24.5942 mL | 49.1884 mL |
| 5 mM | 0.9838 mL | 4.9188 mL | 9.8377 mL |
| 10 mM | 0.4919 mL | 2.4594 mL | 4.9188 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。