Evatanepag (CP-533536) 是一种非前列腺素的，有效的和选择性的EP2受体激动剂。 Evatanepag 可诱导局部骨形成 (in vivo)。Evatanepag 可用于骨折、骨缺损、哮喘的研究。
| 生物活性 | Evatanepag (CP-533536) is a non-prostanoid, potent and selectiveEP2receptoragonist. Evatanepag can induce local bone formationin vivo. Evatanepag can be used in the research of fractures, bone defects, asthma[1][2]. |
体外研究
(In Vitro) | 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 IC50of 50 nM[3].
|
体内研究
(In Vivo) | 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 (t1/2: 0.33 h)[1].
| Animal Model: | Rats[1] | | 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[2] | | 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. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 中文名称 | 2-[3-[N-(4-叔丁基苄基)-N-(吡啶-3-基磺酰基)氨基甲基]苯氧基]乙酸 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
| 溶解性数据 | In Vitro: DMSO : ≥ 32 mg/mL(68.29 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.1342 mL | 10.6708 mL | 21.3415 mL | | 5 mM | 0.4268 mL | 2.1342 mL | 4.2683 mL | | 10 mM | 0.2134 mL | 1.0671 mL | 2.1342 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
m.cnreagent.com