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- 详细信息
- 技术资料
- 保存条件:
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
- 库存:
99
- 供应商:
爱必信(上海)生物科技有限公司
- CAS号:
117946-91-5
- 规格:
5mg/25mg
| 规格: | 5mg | 产品价格: | ¥945.0 |
|---|---|---|---|
| 规格: | 25mg | 产品价格: | ¥3209.0 |
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抑制剂描述: 产品名称:Luzindole 产品别名:见爱必信官网 英文别名:Luzindole 靶点: CAS:117946-91-5 纯度:≥98% 外观:见爱必信官网 保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. 描述: Luzindole is a melatonin receptor antagonist, with a 25-fold higher affinity for the MEL-1B-R over the MEL-1A-R receptor subtype. Melatonin is a hormone produced endogenously from serotonin (5-HT), and melatonin interaction at the MEL-1B-R receptor is thought to represent a chemical underpinning for circadian rhythm and the sleep-wake cycle. Luzindole MEL-1B-R antagonism is described to modulate functions of melatonin signaling and the relationship between melatonin regulation and neurotransmission. Luzindole blocks melatonin-mediated inhibition of forskolin-stimulated cyclic AMP production in CHO cells. At 1μM Luzindole antagonizes the melatonin-elicited inhibition of calcium-dependent dopamine release, and at higher concentrations (from 1μM to 10μM) affects the response of this dopamine release mechanism to melatonin concentrations (shifts the dose-response curve). Melatonin activation of the MEL-1B-R receptor advances the circadian rhythm, and antagonism by Luzindole shows a similar shift in the dose-response curve for the response of biological timing to melatonin concentration, providing evidence that the MEL-1B-R receptor indeed represents a chemical foundation for the circadian timing system. Luzindole significantly antagonizes melatonin-mediated antinociception, suggesting that MEL-1B-R plays a further role as a mediator of melatonin modulation of pain signaling. 溶解性:DMSO : 250 mg/mL (855.08 mM; Need ultrasonic) 体外研究: Luzindole (N-0774) (5-10 μg/ml) inhibits antigen-specific proliferation of the MBP-reactive LV-4 T cell line. 体内研究: Luzindole (N-0774) (30 mg/kg; i.p.; days 0-5) suppresses experimental autoimmune encephalomyelitis.
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