2. Membrane Transporter/Ion Channel Others
  3. Piezo Channel Amino acid Transporter Drug Derivative
  4. Piezo1 agonist 2

Piezo1 agonist 2 (Compound PD2) 是一种可透过血脑屏障的 Piezo1 激动剂，同时也是利用 LAT1 的 Jedi2 (HY-131018) 偶联物。Piezo1 agonist 2 在小鼠体内释放 Jedi2。Piezo1 agonist 2 可用于神经退行性疾病的研究。

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Piezo1 agonist 2

Piezo1 agonist 2 Chemical Structure

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Piezo1 agonist 2 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Piezo1 agonist 2 (Compound PD2) is a blood-brain barrier-permeable Piezo1 agonist and Jedi2 (HY-131018) conjugate that utilizes LAT1. Piezo1 agonist 2 releases Jedi2 in mice. Piezo1 agonist 2 can be used for the research of neurodegenerative diseases[1].

体外研究
(In Vitro)

Piezo1 agonist 2 (PD2) (5 h) 在小鼠血清中的半衰期为 33 ± 1 min，在小鼠肝脏 S9 中的半衰期为 71 ± 1 min[1]。
Piezo1 agonist 2 (PD2) (5-200 μM; 30 min) 在小鼠小胶质细胞 BV2 中呈浓度依赖性摄取，其 Km 为 148 μM[1]。
Piezo1 agonist 2 (PD2) (1-100 μM; 48 h) 在高达 100 μM 的浓度下不会显著降低小鼠小胶质细胞 BV2 的活力，细胞活力维持在未处理对照组的 92 ± 2%以上[1]。

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

Piezo1 agonist 2 相关抗体:
体内研究
(In Vivo)

Piezo1 agonist 2 (15 μmol/kg；腹腔注射；单次推注) 在小鼠中可增强其活性代谢产物 Jedi2 的脑靶向性[1]。

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

Animal Model: C57BL/6JOlaHsd (male, 10 weeks old, 25 ± 5 g)[1]
Dosage: 15 μmol/kg
Administration: i.p.; single bolus injection
Result: Reached a peak plasma concentration (Cmax) of 325.0 nmol/mL at 5 minutes, and a peak brain concentration of 0.64 nmol/g at 15 minutes.
Achieved an area under the curve (AUC) of 66.65 nmol/g × min in brain tissue, with a brain-to-plasma distribution coefficient (Kp) of 0.008.
Released Jedi2 in all studied tissues starting at the 5-minute time point; the released Jedi2 had a brain Kp of 0.175, which was higher than the Kp of directly administered Jedi2 (0.053).
Showed reduced distribution to peripheral tissues compared to Jedi2, with liver Kp 0.09, lungs Kp 0.10, pancreas Kp 0.35, and kidney Kp 0.15.
分子量

371.41

Formula

C19H17NO5S
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

Piezo1 agonist 2 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Piezo1 agonist 2Piezo ChannelAmino acid TransporterDrug Derivative氨基酸转运蛋白Drug derivativeHEK293T cellsneurodegenerative disordersblood-brain barrierhuman plasmaPiezo1mouse liver S9LAT1Jedi2mouse serummouse microglial BV2 cellsInhibitorinhibitorinhibit

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