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• 产品描述： 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

• 靶点： EP2;ProstaglandinReceptor

• 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

• 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.

• 参考文献：
  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. 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. 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.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.134 ml	10.671 ml	21.342 ml
  5 mM	0.427 ml	2.134 ml	4.268 ml
  10 mM	0.213 ml	1.067 ml	2.134 ml
  50 mM	0.043 ml	0.213 ml	0.427 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *