Evatanepag

Research use only, not for human use.

Evatanepag is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation with EC50 of 0.3 nM.

Evatanepag is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation with EC50 of 0.3 nM.CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing.

Evatanepag (10 nM, 30 min) inhibits hFcεRI-induced mast cells degranulation in a dose-dependent manner.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.

Evatanepag (0.3-3.0 mg/kg, directly injected into the marrow cavity of the tibia) promotes bone formation in rats.Evatanepag (0.3, 3.0 mg/kg, intranasal administration, from day1 to day4) reduces HDM aeroallergen-induced increased RL response to methacholine in mice.Evatanepag (1 mg/kg, intravenous injection) demonstrates high i.v. clearance (Cl: 56 mL/min/kg) and a short half-life (t1/2: 0.33 h). Animal Model:Rats Dosage:0.3, 1.0, 3.0 mg/kg Administration:Directly injected into the marrow cavity of the tibia Result:Dose-dependently increased in bone area, bone mineral content, bone mineral density.Animal Model:HDM (house dust mite)-sensitized BALB/c mice Dosage:0.3 mg/kg, 3 mg/kg Administration:Intranasal administration, from day1 to day4.Result:Prevented aeroallergen-driven increased RL (lung resistance) at 0.3 mg/kg. Prevented the enhanced MC activity by approximately 48% at 3 mg/kg.

CP-533536 free acid

GPCR/G Protein

Prostaglandin Receptor

PGE2

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223488-57-1

468.57

C25H28N2O5S

>98% (HPLC)

DMSO:32 mg/mL (68.29 mM)

O=C(O)COC1=CC=CC(CN(CC2=CC=C(C(C)(C)C)C=C2)S(=O)(C3=CC=CN=C3)=O)=C1

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(-20℃)

With Ice Pack

≥ 2 years