产品
编 号:F280788
分子式:C25H28N2O5S
分子量:468.57
产品类型
结构图
CAS No: 223488-57-1
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产品详情
生物活性:
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.
体内研究:
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.
体外研究:
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.