| 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 |
| 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： |
-80℃（运输条件：冰袋低温运输） |
| 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 |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京