1. GPCR/G Protein Neuronal Signaling
  2. Neurokinin Receptor
  3. R116031

R116031 是一种选择性神经激肽-1 (NK-1) 受体拮抗剂,对人 NK-1 受体的 Ki 为 0.45 nM。R116031 可抑制 Substance P (HY-P0201) 诱导的外周效应 (豚鼠的皮肤反应和血浆渗出) 和中枢效应 (沙鼠的捶打行为)。3H 标记的 R116031 可显著蓄积于在沙鼠模型的纹状体、嗅结节、嗅球和蓝斑核。R116031 可用作正电子发射断层扫描 (PET) 配体进行 PET 成像。

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R116031

R116031 Chemical Structure

CAS No. : 336884-84-5

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生物活性

R116031 is a selective Neurokinin-1 (NK-1) receptor antagonist with a Ki of 0.45 nM for human NK-1 receptor. R116031 inhibits Substance P (HY-P0201)-induced peripheral effects (skin reactions and plasma extravasation in guinea pigs) and a central effect (thumping in gerbils).R116031 labeled with 3H significantly accumulate in the striatum, olfactory tubercule, olfactory bulb and locus coeruleus in gerbils models. R116031 can be used as a positron emission tomography (PET) ligand for PET imaging[1].

分子量

660.69

Formula

C35H38F6N4O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
R116031
目录号:
HY-123497
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