1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. 5HT6-ligand-2

5HT6-ligand-2 (compound 15) 是一种有效的 5-HT6 抑制剂,其对 5-HT6 和 SERT 的 Ki 值分别为 3.4 和 15 nM。5HT6-ligand-2 显示出神经保护作用。5HT6-ligand-2 具有用于痴呆症研究的潜力。

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5HT6-ligand-2 Chemical Structure

5HT6-ligand-2 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

5HT6-ligand-2 (compound 15) is a potent 5-HT6 inhibitor with Ki values of 3.4, 15 nM for 5-HT6, SERT, respectively. 5HT6-ligand-2 shows neuroprotection. 5HT6-ligand-2 has the potential for the research of dementia[1].

IC50 & Target[1]

5-HT6 Receptor

 

体内研究
(In Vivo)

BET-IN-26 (compound 13a) (10, 100 mg/kg; p.o.) 以剂量依赖性方式降低小鼠中 LPS (HY-D1056) 诱导的血清 IL-6 和 MCP-1 水平[1]。 药代动力学分析 (2.5 mg/kg; i.p.; Male Wistar rats)[1].

Parameter Serum Brain
Cmax (ng/ml(g)) 45.21 3.78
tmax (min) 30 30
lz (min-1) 0.0099 0.0072
t0.5 (min) 70.08 96.71
Vz/F (l/kg) 55.87 -
CL/F (l/min/kg) 0.55 -
AUC(0-inf) (ng/mL*min) 4542.15 606.48
MRT (min) 104.27 152.35

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

Animal Model: 230-260 g, 8 weeks old Male Wistar rats (MK-801-induced memory impairment)[1]
Dosage: 2.5, 5, 7.5 mg/kg
Administration: I.p.; 30 min before testing
Result: Significantly reduced immobility time by 30.5 % and increased climbing behaviors by 63 %, without affecting the duration of swimming at 5 mg/kg.
分子量

476.57

Formula

C29H28N6O

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:
5HT6-ligand-2
目录号:
HY-162636
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