2. GPCR/G Protein Immunology/Inflammation
  3. Prostaglandin Receptor Interleukin Related
  4. EP4 receptor antagonist 8

EP4 receptor antagonist 8 是一种具有口服活性的 EP4 受体拮抗剂 (人 EP4 IC50 = 6.40 nM)。EP4 receptor antagonist 8 以剂量依赖的方式显著减轻了关节炎 (AIA) 小鼠的爪和关节肿胀、炎症细胞浸润、软骨损伤、血管翳形成以及关节骨侵蚀。EP4 receptor antagonist 8 可用于炎症性疼痛的研究。

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EP4 receptor antagonist 8

EP4 receptor antagonist 8 Chemical Structure

CAS No. : 3068255-86-4

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EP4 receptor antagonist 8 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EP4 receptor antagonist 8 is an orally active EP4 antagonist (human EP4 IC50 = 6.40 nM). EP4 receptor antagonist 8 significantly reduced paw and joint swelling, inflammatory cell infiltration, cartilage damage, pannus formation, and joint bone erosion in arthritis (AIA) mice in a dose-dependent manner. EP4 receptor antagonist 8 can be used for the study of inflammatory pain[1].

IC50 & Target

EP4

6.4 nM (IC50)

IL-6

 

体外研究
(In Vitro)

EP4 receptor antagonist 8 (Compound 27i) (100 μg/mL，0-60 分钟) 在大鼠肝微粒体 (RLM) 中的代谢稳定性随时间推移而降低，60 分钟时剩余百分比为 41.44 %[1]。
EP4 receptor antagonist 8 (24 小时) 在 24 小时表现出中等的血浆蛋白结合率 (97.60 %)[1]。
EP4 receptor antagonist 8 以剂量依赖的方式显著降低脂多糖 (HY-D1056) (LPS) 诱导的 RAW 264.7 细胞中的 IL-6 水平[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

EP4 receptor antagonist 8 相关抗体:

ELISA Assay[1]

Cell Line: Lipopolysaccharides (LPS)-induced RAW 264.7 cells
Concentration: 6.25 μM, 12.5 μM, 25 μM, 50 μM
Incubation Time: Pretreated 1 h, then simulated with LPS for 24 h
Result: Reduced LPS-induced IL-6 levels in a dose-dependent manner.
体内研究
(In Vivo)

EP4 receptor antagonist 8 (Compound 27i) (5-20 mg/kg，腹腔注射，单次给药，在 CFA 注射后 24 小时给药) 在弗氏完全佐剂 (CFA) 诱导的 C57BL/6 小鼠关节炎模型中表现出显著的抗炎和镇痛作用，且呈剂量依赖性[1]。
EP4 receptor antagonist 8 (5-20 mg/kg，口服，每日一次，连续 5 天) 在昆明小鼠急性炎症模型中表现出强效的抗炎活性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Chronic arthritis was induced in the right hind paw using C57BL/6 mice (female, weighing 20-22 g) by injection of complete Freund's adjuvant (CFA)[1].
Dosage: 5 mg/kg, 10 mg/kg, 20 mg/kg
Administration: I.p., once, performed 24 hours after CFA injection
Result: Significantly improved the swelling of mice paws in a dose-dependent manner.
Increased the pain threshold; in both the hot plate test and the Von Frey test, the 20 mg/kg group showed the best effect within 120 minutes.
Reduced joint inflammation, cartilage damage, bone erosion, and pannus formation.
Reduced IL-1β, IL-6, and TNF-α positive cells in joint tissue.
Animal Model: Acute ear inflammation and swelling were induced in male Kunming mice (weighing 20-22 g) by uniformly applying xylene (20 μL) to the right ear[1].
Dosage: 5 mg/kg, 10 mg/kg, 20 mg/kg
Administration: P.o., once daily for 5 days
Result: Showed excellent inhibitory effect, and the inhibitory rate was as high as 47.09 %, which was dose-dependent.
分子量

516.94

Formula

C26H21ClN6O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

EP4 receptor antagonist 8 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EP4 receptor antagonist 83068255-86-4Prostaglandin ReceptorInterleukin RelatedILAnalgesic activityAnti-inflammatoryEP4 antagonistsStructure activity relationshipInhibitorinhibitorinhibit

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