P2Y14R antagonist 3
P2Y14R antagonist 3 (Compound A) is a potent and orally active P2Y14R antagonist with an IC50 value of 23.60 nM and a Kd value of 7.26 μM. P2Y14R antagonist 3 can reduce the degree of lung injury in the Lipopolysaccharides (LPS) (HY-D1056)-induced acute lung injury mice. P2Y14R antagonist 3 can be used for inflammatory diseases.
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- Formel: C26H25N5O5
- Molecular Weight:487.51
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
P2Y14 Receptor 23.6 nM (IC50) |
P2Y14 Receptor 7.26 μM (Kd) |
In Vitro
P2Y14R antagonist 3 exhibits no inhibitory effect on CYP1A2 and CYP2C9, and weak inhibitory activity against CYP2C19 and CYP3A4, with IC50 values of 28.6 μM and 21.3 μM, respectively[1].
P2Y14R antagonist 3 does not exhibits cardiotoxic side effects, exhibits exceptional biopharmaceutical stability, demonstrating resistance to degradation in simulated gastric fluid and intestinal fluid, maintaining high metabolic stability in human liver microsomes, classify it as a low-clearance compound[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LPS-induced acute lung injury male C57BL/6 mice (6-8 weeks)[1]
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Dosage:2 mg/kg, 6 mg/kg
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Administration:Oral gavage (p.o.); once daily for 7 days, on the 5th day of the experiment, mice were injected with 25 mg/kg LPS to induce Acute Lung Injury (ALI), and mice were killed 3 h after 7th day administration.
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Result:Reduced inflammation and reduced tissue damage, and reduced the content of inflammatory cytokines and the pathological changes of lung tissue in LPS-induced ALI mouse model.
Chemical Information
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Molecular Weight 487.51
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Formel C26H25N5O5
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SMILES
CNC(C1CN(CC12CCN(CC2)C(C3=NOC4=CC=CC=C43)=O)C(C5=C6C=CC=CC6=NO5)=O)=O
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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.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Inhalation Toxicity Study
Inhalation toxicity studies expose rodents to a controlled aerosol, vapor, gas, or smoke atmosphere and assess respiratory and systemic toxicity using exposure-atmosphere characterization, clinical observations, body and organ weights, bronchoalveolar lavage fluid, histopathology, blood chemistry, hematology, and, when included, molecular endpoints such as transcriptomics, proteomics, lipidomics, or tissue burden analysis. The primary biological readouts are airway irritation, pulmonary inflammation, cytotoxicity, altered surfactant or lipid homeostasis, impaired particle clearance, and tissue remodeling, reflected by BALF cell differentials, BALF protein, LDH, phosphatase activities, cytokines, lung weight, microscopic respiratory-tract lesions, and retained lung burden.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)