Piezo1 agonist 2 hydrochloride
Based on 1 Customer Validation
Piezo1 agonist 2 hydrochloride is a blood-brain barrier-permeable Piezo1 agonist and Jedi2 (HY-131018) conjugate that utilizes LAT1. Piezo1 agonist 2 hydrochloride releases Jedi2 in mice. Piezo1 agonist 2 hydrochloride can be used for the research of neurodegenerative diseases.
For research use only. We do not sell to patients.
- Formula: C19H18ClNO5S
- Molecular Weight:407.87
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
The half-life of Piezo1 agonist 2 (PD2) (5 h) hydrochloride is 33 min in mouse serum and 71 min in mouse liver S9[1].
Piezo1 agonist 2 (5-200 μM; 30 min) hydrochloride is taken up in a concentration-dependent manner by mouse microglial BV2 cells, with a Km value of 148 μM[1].
Piezo1 agonist 2 (1-100 μM; 48 h) hydrochloride does not significantly reduce the viability of mouse microglial BV2 cells at concentrations up to 100 μM, with cell viability remaining above 92 % of that in the untreated control group[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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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Molecular Weight 407.87
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Formula C19H18ClNO5S
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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.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (122.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4518 mL | 12.2588 mL | 24.5176 mL | 61.2940 mL |
| 5 mM | 0.4904 mL | 2.4518 mL | 4.9035 mL | 12.2588 mL | |
| 10 mM | 0.2452 mL | 1.2259 mL | 2.4518 mL | 6.1294 mL | |
| 15 mM | 0.1635 mL | 0.8173 mL | 1.6345 mL | 4.0863 mL | |
| 20 mM | 0.1226 mL | 0.6129 mL | 1.2259 mL | 3.0647 mL | |
| 25 mM | 0.0981 mL | 0.4904 mL | 0.9807 mL | 2.4518 mL | |
| 30 mM | 0.0817 mL | 0.4086 mL | 0.8173 mL | 2.0431 mL | |
| 40 mM | 0.0613 mL | 0.3065 mL | 0.6129 mL | 1.5324 mL | |
| 50 mM | 0.0490 mL | 0.2452 mL | 0.4904 mL | 1.2259 mL | |
| 60 mM | 0.0409 mL | 0.2043 mL | 0.4086 mL | 1.0216 mL | |
| 80 mM | 0.0306 mL | 0.1532 mL | 0.3065 mL | 0.7662 mL | |
| 100 mM | 0.0245 mL | 0.1226 mL | 0.2452 mL | 0.6129 mL |