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

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.

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Piezo1 agonist 2

Piezo1 agonist 2 Chemical Structure

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Piezo1 agonist 2 Related Antibodies

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Description

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].

In Vitro

The half-life of Piezo1 agonist 2 (PD2) (5 h) is 33 ± 1 min in mouse serum and 71 ± 1 min in mouse liver S9[1].
Piezo1 agonist 2 (PD2) (5-200 μM; 30 min) is taken up in a concentration-dependent manner by mouse microglial BV2 cells, with a Km value of 148 μM[1].
Piezo1 agonist 2 (PD2) (1-100 μM; 48 h) does not significantly reduce the viability of mouse microglial BV2 cells at concentrations up to 100 μM, with cell viability remaining above 92 ± 2% of that in the untreated control group[1].

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

Piezo1 agonist 2 Related Antibodies
In Vivo

Piezo1 agonist 2 (15 μmol/kg; i.p.; single bolus injection) enhances the brain targeting of its active metabolite Jedi2 in mice[1].

MedChemExpress (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.
Molecular Weight

371.41

Formula

C19H17NO5S
SMILES

O=C(O)[C@@H](N)CC1=CC=CC(OC(C2=C(C)OC(C3=CC=CS3)=C2)=O)=C1
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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Piezo1 agonist 2 Related Classifications

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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.

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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