1. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  2. Glycine Receptor (GlyR) 5-HT Receptor
  3. PSN09

PSN09 是一种能透过血脑屏障的 PSAM4-GlyRPSAM4-5-HT3 受体激动剂,具有高亲和力。18F 标记的 PSN09 可作为放射性配体用于非人灵长类动物 PET 成像。

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PSN09

PSN09 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

PSN09 is a blood-brain barrier-permeable agonist of PSAM4-GlyR and PSAM4-5-HT3 receptors with high affinity. 18F-labeled PSN09 serves as a radiotracer for PET imaging in non-human primates[1].

IC50 & Target[1]

5-HT3 Receptor

 

体外研究
(In Vitro)

PSN09 可在转染的 HEK-293 细胞中强效结合 PSAM4-GlyR,其 Ki 为 1.86 nM[1]
PSN09 在转染的 HEK-293 细胞中能强效结合 PSAM4-5-HT3,其 Ki 为 5.67 nM[1]
PSN09 (0.1-100 μM) 可在转染的 HEK-293 细胞中强效激活 PSAM4-GlyR,其 EC50 为 8.3 nM[1]
PSN09 (0.1-100 μM) 可在转导的 HEK-293 细胞中强效激活 PSAM4-5-HT3,其 EC50 为 16.8 nM[1]

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

体内研究
(In Vivo)

PSN09 (1 mg/kg; i.v.; single dose) 可激活 PSAM4-GlyR,从而在转导后的恒河猴中诱导神经元抑制[1]

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

Animal Model: Monkey transduced with PSAM4-GlyR (11-year-old male, Lenti-hSyn-PSAM4-GlyR injected into left amygdala)[1]
Dosage: 1 mg/kg
Administration: i.v.; single dose; administered 10 minutes before [18F]FDG injection
Result: Did not significantly alter [18F]FDG arterial input functions.
Reduced MRGlu in the target transduced left amygdala by 19%, and decreased the target-to-mirror MRGlu ratio by 3%.
分子量

335.37

Formula

C20H18FN3O

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:
PSN09
目录号:
HY-181351
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