2. Immunology/Inflammation
  3. Complement System
  4. C5aR1 antagonist 1

C5aR1 antagonist 1 (compound 7e) 是口服有效的 C5aR 拮抗剂。C5aR1 antagonist 1 在 DISCO 和迁移测定中有效，IC50 值分别为 38 nM 和 17 nM。C5aR1 antagonist 1 可用于急慢性炎症性疾病的研究。

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C5aR1 antagonist 1 Chemical Structure

C5aR1 antagonist 1 Chemical Structure

CAS No. : 2365325-67-1

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C5aR1 antagonist 1 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

C5aR1 antagonist 1 (Compound 7e) is an orally active C5a receptor 1 (C5aR1) antagonist. C5aR1 antagonist 1 is active in DISCO and migration assays, with IC50 values of 38 nM and 17 nM, respectively. C5aR1 antagonist 1 can be used for the research of acute and chronic inflammatory diseases[1].

IC50 & Target

C5aR1

 

体外研究
(In Vitro)

C5aR1 antagonist 1 (compound 7e) (10 μM, 2 h) 是 C5aR 的竞争性拮抗剂，KD 值为 15 nM[1]。

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

C5aR1 antagonist 1 相关抗体:
体内研究
(In Vivo)

C5aR1 antagonist 1 (compound 7e) (10/30/50 mg/kg, 单次口服) 在大鼠、狗和食食猴体内的药代动力学特征表明它的低溶解度限制了暴露[1]。
C5aR1 antagonist 1 (1/3/10 mg/kg, 取样检测前2/8/16小时口服) 可剂量依赖性地抑制中性粒细胞增多症大鼠模型的血中性粒细胞增加[1]。
C5aR1 antagonist 1 (0/1/3/10/30 mg/kg, 取样检测前2小时口服) 抑制雌性 hC5aR1 敲入大鼠 CD11b 上调约 90%。[1]。

药代动力学分析[1]

Animals Route Dose (mg/kg) CL mL/(min×kg) Vss_obs (L/kg) T1/2 (h) AUC0‑last (ng×h)/mL Cmax (ng×h)/mL Tmax (h)
rat p.o. 10 39 7.1 4.1 32200 3890 2
dog p.o. 30 2.3 7.6 1.1 14900 2530 1
monkey p.o. 50 3500 635 2 41900 3940 4

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

Animal Model: Neutrophilia Rat Model[1]
Dosage: 1/3/10 mg/kg
Administration: Oral gavage (p.o.), Rats were administered po with compound or vehicle at 23.5/15.5/7.5/1.5 h before hC5a iv injection.
Result: Inhibited reactive neutrophilia induced by hC5a administration in vivo.
分子量

497.53

Formula

C28H27F4N3O
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

C5aR1 antagonist 1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

C5aR1 antagonist 12365325-67-1Complement SystemHumanized C5aR1 RatsC5aR1 Knockout RatsInflammationNeutrophilia Rat ModelInhibitorinhibitorinhibit

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