Evatanepag  (Synonyms: CP-533536 free acid)

Evatanepag (CP-533536) is a non-prostanoid, potent and selective EP₂ receptor agonist. Evatanepag can induce local bone formation in vivo. Evatanepag can be used in the research of fractures, bone defects, asthma^[1][2].

Evatanepag (10 nM, 30 min) inhibits hFcεRI-induced mast cells degranulation in a dose-dependent manner^[2].
Evatanepag (0.1 nM-10 μM, 12 min) results in an equivalent increase in intracellular cAMP in HEK-293 cells, with an IC₅₀ of 50 nM^[3].

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

Evatanepag (0.3-3.0 mg/kg, directly injected into the marrow cavity of the tibia) promotes bone formation in rats^[1].
Evatanepag (0.3, 3.0 mg/kg, intranasal administration, from day1 to day4) reduces HDM aeroallergen-induced increased RL response to methacholine in mice^[2].
Evatanepag (1 mg/kg, intravenous injection) demonstrates high i.v. clearance (Cl: 56 mL/min/kg) and a short half-life (t_1/2: 0.33 h)^[1].

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

468.57

Solid

C₂₅H₂₈N₂O₅S

223488-57-1

CC(C)(C)C(C=C1)=CC=C1CN(S(C2=CN=CC=C2)(=O)=O)CC3=CC(OCC(O)=O)=CC=C3

Room temperature in continental US; may vary elsewhere.

• [1]. Cameron KO, et al. Discovery of CP-533536: an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation. Bioorg Med Chem Lett. 2009 Apr 1;19(7):2075-8.  [Content Brief]

  [2]. Judith Plaza, et al. In Vitro and In Vivo Validation of EP2-Receptor Agonism to Selectively Achieve Inhibition of Mast Cell Activity. Allergy Asthma Immunol Res. 2020 Jul;12(4):712-728.  [Content Brief]

  [3]. V M Paralkar, et al. An EP2 receptor-selective prostaglandin E2 agonist induces bone healing. Proc Natl Acad Sci U S A. 2003 May 27;100(11):6736-40.  [Content Brief]