Evatanepag (CP-533536) is a non-prostanoid, potent, and selective EP2 receptor agonist. It induces local bone formation in vivo and can be utilized in research related to fractures, bone defects, and asthma [1][2].
体内研究
Evatanepag (administered directly into the marrow cavity of the tibia at doses ranging from 0.3 to 3.0 mg/kg) stimulates bone formation in rats [1].
Evatanepag (administered intranasally at doses of 0.3 and 3.0 mg/kg from day 1 to day 4) attenuates the augmented RL response to methacholine induced by HDM aeroallergen in mice [2].
Evatanepag (1 mg/kg, intravenous injection) exhibits high i.v. clearance (Cl: 56 mL/min/kg) and a short half-life (t1/2: 0.33 h) [1].
体外研究
Evatanepag (at a concentration of 10 nM for 30 minutes) suppresses hFcεRI-induced mast cell degranulation in a dose-dependent manner [2].
Evatanepag (ranging from 0.1 nM to 10 μM for 12 minutes) induces a comparable elevation in intracellular cAMP levels in HEK-293 cells, exhibiting an IC50 of 50 nM [3].
Evatanepag 细胞实验
Cell Line
Concentration
Treated Time
Description
References
RAW 264.7 macrophages
25 μM
24 hours
To evaluate the inhibitory effect of ethyl gallate on nitric oxide production in LPS-stimulated RAW 264.7 cells. Results showed that ethyl gallate significantly inhibited NO production at 25 μM.
PLoS One. 2018 Nov 28;13(11):e0207872
Rat basophilic leukemia humanized cell line RS-ATL8
10^-12 M to 10^-4 M
30 minutes
To evaluate the inhibitory effect of Evatanepag on RS-ATL8 cell degranulation. Results showed Evatanepag inhibited hFcεRI-induced mast cell degranulation in a dose-dependent manner from 10^-12 M to 10^-8 M, with a maximum inhibition rate of 46%.
To evaluate the inhibitory effect of Evatanepag on LAD2 cell degranulation. Results showed Evatanepag inhibited FcεRI-induced mast cell degranulation in a dose-dependent manner, with a maximum inhibition rate of 37.2%.
To evaluate the protective effect of Evatanepag in a house dust mite-induced asthma model. Results showed 0.3 mg·kg^-1 dose significantly reduced airway hyperresponsiveness, while 3 mg·kg^-1 dose reduced airway mast cell activity by 48% (not statistically significant).
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