S82515 |
PNU-282987 |
源叶(MedMol) | 99% |
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- 产品描述: PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 can be used for the research of central and peripheral nervous systems
- 靶点: IC50: 4541nM (5-HT3); EC50: 154 nM (α7 nAChR); Ki: 27 nM (R7 MLA);AChR
- 体外研究:
PNU-282987 (Compound C7) displaces the R7 selective antagonist methyllycaconitine (MLA) from rat brain homogenates with a Ki of 27 nM. PNU-282987 has α7 nAChR agonist activity with an EC50 of 154 nM. PNU-282987 also has inhibition for the 5-HT3 receptor with an IC50 value of 4541nM
- 体内研究:
PNU-282987 (Compound C7) (i.v.; 1, 3 mg/kg) leads to a reversal of the gating deficit. PNU-282987 (30 μM) evokes currents in rat hippocampal neurons in a concentration-dependent and MLA blockable manner. Animal Model: Rats Dosage: 1, 3 mg/kg Administration: i.v. Result: Significantly reversed amphetamine-induced gating deficit.
- 参考文献:
1. Alice L Bodnar, et al. Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors. J Med Chem. 2005 Feb 24;48(4):905-8.
- 溶解性: Soluble in DMSO、H2O
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 3.777 ml 18.886 ml 37.771 ml 5 mM 0.755 ml 3.777 ml 7.554 ml 10 mM 0.378 ml 1.889 ml 3.777 ml 50 mM 0.076 ml 0.378 ml 0.755 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)