Mardepodect
(Synonyms: 2-[[4-[1-甲基-4-(4-吡啶基)-1H-吡唑-3-基]苯氧基]甲基]-喹啉,PF-2545920) 目录号 : GC36540
A potent inhibitor of PDE10A
Cas No.:898562-94-2
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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
PF-2545920 is a potent inhibitor of phosphodiesterase 10A (PDE10A; IC50 = 1.26 nM for the human recombinant enzyme).1 It is selective for PDE10A over other PDEs with IC50 values ranging from 1.7 to >10 μM. In vivo, PF-2545920 (0.1-3 mg/kg, i.p.) increases cAMP and cGMP production as well as phosphorylation of CREB and GluR1 in mouse striatum in a dose-dependent manner. It reduces climbing behavior induced by apomorphine in mice (ID50 = 0.375 mg/kg) and disrupts the conditioned avoidance response in mice and rats (ID50s = 0.441 and 1.079 mg/kg, respectively). PF-2545920 reverses deficits in prepulse inhibition and social odor recognition induced by (+)-MK-801 in rats. Formulations containing PF-2545920 are under clinical investigation for the treatment of schizophrenia and Huntington's disease.
1.Grauer, S.M., Pulito, V.L., Navarra, R.L., et al.Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophreniaJ. Pharmacol. Exp. Ther.331(2)574-590(2009)
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5481 mL | 12.7405 mL | 25.481 mL |
| 5 mM | 0.5096 mL | 2.5481 mL | 5.0962 mL |
| 10 mM | 0.2548 mL | 1.274 mL | 2.5481 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。