P2Y14R antagonist 3

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P2Y14R antagonist 3 (Compound A) is a potent and orally active P2Y₁₄R antagonist with an IC₅₀ value of 23.60 nM and a K_d 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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P2Y14R antagonist 3 Chemical Structure

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

In Vivo

P2Y14R antagonist 3 (2-6 mg/kg; p.o.; once daily for 7 days) can reduce the degree of lung injury in the LPS-induced acute lung injury mice, and the infiltration of immune cells is decreased, the level of inflammatory factors IL-6, TNF-α and IL-β are considerably decreased^[1].

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

Animal Model:	LPS-induced acute lung injury male C57BL/6 mice (6-8 weeks)^[1]
Dosage:	2 mg/kg, 6 mg/kg
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.
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.

Molecular Weight

487.51

Formula

C₂₆H₂₅N₅O₅

SMILES

CNC(C1CN(CC12CCN(CC2)C(C3=NOC4=CC=CC=C43)=O)C(C5=C6C=CC=CC6=NO5)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Wei Z, et al. Discovery of a potent and in vivo anti-inflammatory Efficacious, P2Y14R antagonist with a novel benzisoxazoles scaffold by DNA-encoded chemical library technology. Eur J Med Chem. 2025 Feb 27;289:117451. [Content Brief]

[2]. Mourad MAE, et al. Novel inhibitors of oncogenic Wnt/TCF-4/-catenin signaling pathway: Design, synthesis, molecular docking studies and apoptosis inducing activity of pyrimidothiazino-, dihydropyrimidotriazepino- and 1,3,4-thiadiazolopyrimido-indole hybrids. Bioorg Chem. 2025 Feb 26;157:108285. [Content Brief]