BMS-986187,98.93%
产品编号:Bellancom-120613| CAS NO:684238-37-7| 分子式:C31H34O4| 分子量:470.60
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BMS-986187
产品介绍 | BMS-986187 是一种 δ 阿片受体选择性正变构调节剂 (PAM),EC50 为 0.03 μM,pKB 为 6.02 (~1 μM)。BMS-986187 在 μ 受体上没有可观察到的 PAM 活性 (EC50=3 μM)。 | ||||||||||||||||
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生物活性 | BMS-986187 is an δ-opioid receptor-selective positive allosteric modulator (PAM) with an EC50 of 0.03 μM and a pKB of 6.02 (∼1 μM). BMS-986187 has no observable PAM activity at the μ-receptor (EC50=3 μM). | ||||||||||||||||
体外研究 |
BMS-986187 (1 nM-100 uM) produces little or no activity in agonist mode, but in PAM mode (in the presence of an EC20 of leu-enkephalin (in CHO-OPRD1 cells) or endomorphin 1 (in CHO-OPRM1 cells)) produces a response with an EC50 of 48 nM in CHO-OPRD1 cells and 2 μM in CHO-OPRM1 cells. 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
体内研究 | |||||||||||||||||
体内研究 | |||||||||||||||||
性状 | Solid | ||||||||||||||||
溶解性数据 |
In Vitro:
DMSO : 25 mg/mL (53.12 mM; Need ultrasonic) 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) | ||||||||||||||||
参考文献 |