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P2Y14R antagonist 3 (compound A) is an orally active P2Y14R antagonist with an IC50 of 23.60 nM and a Kd of 7.26 μM. It mitigates lung injury in mice induced by Lipopolysaccharides (LPS) and can be utilized in the study of inflammatory diseases.
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Description | P2Y14R antagonist 3 (compound A) is an orally active P2Y14R antagonist with an IC50 of 23.60 nM and a Kd of 7.26 μM. It mitigates lung injury in mice induced by Lipopolysaccharides (LPS) and can be utilized in the study of inflammatory diseases. |
Targets&IC50 | P2Y14 Receptor:7.26 μM(Kd) |
In vitro | P2Y14R antagonist 3 does not inhibit CYP1A2 and CYP2C9, but exhibits weak inhibitory activity against CYP2C19 and CYP3A4 with IC 50 values of 28.6 μM and 21.3 μM, respectively [1]. This compound shows no cardiotoxic side effects and demonstrates excellent biopharmaceutical stability, resisting degradation in simulated gastric and intestinal fluids. It also maintains high metabolic stability in human liver microsomes, categorizing it as a low-clearance compound [1]. |
In vivo | The administration of P2Y14R antagonist 3 (2–6 mg/kg; oral administration; once daily for 7 consecutive days) mitigates the severity of lung injury in mice induced by LPS, leading to reduced immune cell infiltration and significantly lower levels of inflammatory factors IL-6, TNF-α, and IL-1β. |
Molecular Weight | 487.51 |
Formula | C26H25N5O5 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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