1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
    Adrenergic Receptor
  3. ST1936 oxalate

ST1936 oxalate 

目录号: HY-103110A
产品使用指南

ST1936 oxalate 是一种选择性的纳摩尔亲和力的 5-HT6 受体激动剂,对人 5-HT6、5-HT7 和 5-HT2B 受体的 Ki 值分别为 13 nM,168 nM 和 245 nM。ST1936 oxalate 对人和大鼠的 α2 肾上腺素受体也显示出中等亲和力 (Ki 为 300 nM)。

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ST1936 oxalate Chemical Structure

ST1936 oxalate Chemical Structure

CAS No. : 1782228-83-4

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生物活性

ST1936 oxalate is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor[1].

IC50 & Target[1]

5-HT6 Receptor

13 nM (Ki)

Human 5-HT7 Receptor

168 nM (Ki)

5-HT2B Receptor

245 nM (Ki)

α1-adrenergic receptor

390 nM (Ki, rat)

α2-adrenergic receptor

300 nM (Ki, rat)

α2-adrenergic receptor

300 nM (Ki, human)

体外研究
(In Vitro)

ST1936 oxalate appears to be relatively selective for 5-HT6 receptors, although it has shown affinity also for 5-HT2B, 5-HT1A, 5-HT7 receptor and α-adrenergic receptors when tested in a broad crossreactivity panel that comprised G-protein-coupled receptors, ion channel binding sites, enzymes, and transporters[1].
ST1936 oxalate behaves as a full 5-HT6 agonist on cloned cells and is able to increase Ca2+ concentration, phosphorylation of Fyn kinase, and regulate the activation of ERK1/2 that is a downstream target of Fyn kinase[2].
ST1936 oxalate reduces the frequency of spontaneous excitatory postsynaptic currents, with an IC50 of 1.3 μM[3].

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

体内研究
(In Vivo)

ST1936 (5, 10, 20 mg/kg; i.p.) oxalate increases in a dose dependent manner extracellular dopamine (DA) and NA levels in the prefrontal cortex (PFCX)[2].
ST1936 (5, 10, 20 mg/kg; i.p.) oxalate increases extracellular DA and NA levels in the nucleus accumbens (NAc) core. Doses of 10 mg/kg increases dialysate DA (peak: 179%) while higher dose increases both DA and NA dialysates (201% and 231%, respectively). Doses of 5 mg/kg does not produce any effect[2].

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

分子量

326.78

Formula

C15H19ClN2O4

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.

参考文献
  • 摩尔计算器

  • 稀释计算器

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ST1936 oxalate
目录号:
HY-103110A
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