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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- CAS. Nr.: 3124796-49-9
- Formel: C19H17NO5S
- Molecular Weight:371.41
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
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Help & FAQs
Biologische Aktivität
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6JOlaHsd (male, 10 weeks old, 25 ± 5 g)[1]
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Dosage:15 μmol/kg
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Administration:i.p.; single bolus injection
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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.
Chemical Information
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CAS. Nr. 3124796-49-9
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Molecular Weight 371.41
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Formel C19H17NO5S
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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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Piezo1 agonist 2 Related Classifications
HY-181743 Related Classifications
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