| 产品描述： | JP1302 dihydrochloride is a potent, selective, high affinity antagonist of the α2C-adrenoceptor, with a Kb of 16 nM and a Ki of 28 nM for the human α2C-receptor. JP1302 dihydrochloride shows antidepressant and antipsychotic-like effects. JP1302 dihydrochloride can be used for neuropsychiatric disorders and renal dysfunction research |
| 靶点： |
human α2C-adrenoceptor:28±2 nM (Ki);human α2B-adrenoceptor:1470±130 nM (Ki);human α2A-adrenoceptor:3150±50 nM (Ki);rodent α2D-adrenoceptor:1700±200 nM (Ki) |
| 体内研究： |
JP1302 (1-10 μmol/kg) decreases immobility time in the FST to a level similar to that seen with 10-30 μmol/kg of the antidepressant Desipramine (HY-B1272A). JP1302 (5 μmol/kg, once) is capable of complete reversal of the impairment in PPI induced in Sprague-Dawley rats by the psychotomimetic NMDA receptor antagonist, phencyclidine and similar results are found in Wistar rats. JP1302 (3 mg/kg, IV, once) significantly ameliorates renal dysfunction. Animal Model: Male Sprague Dawley rats (8 weeks old) Dosage: 3 mg/kg Administration: IV, pre-treatment: administered 5 min before the induction of ischemia, post-treatment: injected 45 min after the initiation of reperfusion Result: Significantly ameliorated renal dysfunction in the rats at 24 h after reperfusion. post-ischemic administration of JP-1302 significantly ameliorated renal dysfunction, histo logical damage and reduced apoptotic cells and pro-inflammatory cytokine mRNA expression. |
| 参考文献： |
1. Tricklebank MD, et al. JP-1302: a new tool to shed light on the roles of alpha2C-adrenoceptors in brain. Br J Pharmacol. 2007 Feb;150(4):381-2. 2. Sallinen J, et al. Pharmacological characterization and CNS effects of a noel highly selective alpha2C-adrenoceptor antagonist JP-1302. Br J Pharmacol. 2007 Feb;150(4):391-402. 3. Shimokawa T, et al. Post-treatment with JP-1302 protects against renal ischemia/reperfusion-induced acute kidney injury in rats. J Pharmacol Sci. 2019 Mar;139(3):137-142. |
| 溶解性： |
Soluble in DMSO、H2O |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 备注： |
JP1302 dihydrochloride 是选择性的、高亲和力的α2C 肾上腺受体 (α2C-adrenoceptor) 的拮抗剂，其Kb 值为 16 nM，Ki 值为 28 nM。 |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.47 ml |
12.348 ml |
24.695 ml |
| 5 mM |
0.494 ml |
2.47 ml |
4.939 ml |
| 10 mM |
0.247 ml |
1.235 ml |
2.47 ml |
| 50 mM |
0.049 ml |
0.247 ml |
0.494 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京