| 产品描述: | PSEM 89S TFA is a selective and brain penetrant agonists for the resulting ion channels. PSEM 89S TFA is orthogonally selective for Q79G and L141F, respectively |
| 靶点: |
nAChR |
| 体外研究: |
PSEM 89S (10 or 30μM) activates layer 2/3 cortical neurons expressing (Pharmacologically Selective Actuator Module) PSAML141F,Y115F-5HT3 high conductance (HC).
PSEM 89S (10 μM) reversibly silenced transfected neurons by reducing cellular input resistance. |
| 体内研究: |
PSEM 89S strongly reduces photostimulation-evoked feeding in mice expressing PSAML141F,Y115F- glycine receptor (GlyR) (30 mg/kg) but not in mice expressing only channelrhodopsin-2 (ChR2) (50 mg/kg).
PSEM 89S (30 mg/kg) shows good brain penetrance in mice after minimally invasive intraperitoneal administration. Animal Model: Male Agrp-cre mice (3-6 weeks) Dosage: 30 mg/kg Administration: I.p. administration Result: Almost completely suppressed fos (a marker of neuron activation) in ChR2-expressing neurons. Animal Model: C57BL/6 mice Dosage: 30 mg/kg (Pharmacokinetic Analysis) Administration: I.p. administration Result: Rised rapidly in serum and brain, and was mostly cleared from both compartments in 1 h. |
| 参考文献: |
1. Christopher JM, et, al. Chemical and genetic engineering of selective ion channel-ligand interactions. Science. 2011 Sep 2; 333(6047): 1292-6. |
| 溶解性: |
Soluble in DMSO、H2O |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.473 ml |
12.365 ml |
24.729 ml |
| 5 mM |
0.495 ml |
2.473 ml |
4.946 ml |
| 10 mM |
0.247 ml |
1.236 ml |
2.473 ml |
| 50 mM |
0.049 ml |
0.247 ml |
0.495 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |