1. GPCR/G Protein Neuronal Signaling
  2. Somatostatin Receptor
  3. J-2156

J-2156 是一种高效,选择性的生长抑素受体 4 型 (SST4) 激动剂,对于人和大鼠 SST4 受体的 IC50 分别为 0.05 nM 和 0.07 nM。J-2156 用于缓解大鼠同侧后爪的机械性异常性疼痛和机械性痛觉过敏。

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J-2156

J-2156 Chemical Structure

CAS No. : 848647-56-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats[1][2].

IC50 & Target

IC50: 0.05 nM (human SST4) and 0.07 nM (rat SST4)[1]

体外研究
(In Vitro)

J-2156 binds with nanomolar affinity to the human somatostatin receptor subtype 4 (h sst4: Ki=1.2 nM) and is over 400-fold subtype-selective against the other somatostatin receptors (h sst1: Ki=1.2 nM; h sst2: Ki>5000 nM; h sst3: Ki=1400 nM; h sst5: Ki=540 nM) in Chinese hamster ovary (CHO) cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

J-2156 (1-10 mg/kg; i.p.; for 3 hours) of single bolus doses has anti-allodynic effect on ipsilateral and contralateral in BCIBP-rats[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Breast cancer-induced bone pain (BCIBP)-rats[1]
Dosage: 1, 3, 10 mg/kg
Administration: IP; for 3 hours
Result: Had anti-allodynic effect on ipsilateral and contralateral in BCIBP-rats.
分子量

468.57

Formula

C24H28N4O4S

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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Help & FAQs
  • 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:
J-2156
目录号:
HY-111615
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