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

C5aR1 antagonist 2 (Compound 6a) 是一种口服活性 C5a 受体 1 (C5aR1) 拮抗剂，可有效抑制 C5a 诱导的中性粒细胞计数增加。C5aR1 antagonist 2 在 DISCO 和迁移测定中有效，IC50 值分别为 21 和 3 nM。C5aR1 antagonist 2 可用于急慢性炎症性疾病的研究。

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C5aR1 antagonist 2 Chemical Structure

C5aR1 antagonist 2 Chemical Structure

CAS No. : 2365161-92-6

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C5aR1 antagonist 2 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 2 (Compound 6a) is an orally active C5a receptor 1 (C5aR1) antagonist that shows efficacy in inhibiting the C5a-induced neutrophil count increase. C5aR1 antagonist 2 is potent in the DISCO and migration assays, with IC50 values of 21 and 3 nM, respectively. C5aR1 antagonist 2 can be used for the research of acute and chronic inflammatory diseases[1].

体内研究
(In Vivo)

C5aR1 antagonist 2 (1-10 mg/kg, 口服, 一次) 以剂量依赖性方式完全抑制 C5a 诱导的中性粒细胞增多大鼠模型中的 CD11b 上调[1]。
C5aR1 antagonist 2 (1-10 mg/kg, 口服, 一次) 可抑制 Sprague−Dawley 雌性 hC5aR1 敲除大鼠中 C5a 诱导的中性粒细胞增多[1]。

药代动力学分析[1]

Route Dose (mg/kg) AUC0-last (ng·h/mL) Cmax (ng/mL) Tmax (h) CL(mL/(min*kg)) Vss_obs (L/kg) t1/2 (h)
p.o. 10 35700 3610 2.5 39 7.1 3.7

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

509.56

Formula

C29H30F3N3O2
CAS 号
Unlabeled CAS

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 2 相关分类

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Keywords:

C5aR1 antagonist 22365161-92-6Complement SystemDISCOmigrationneutrophilinflammatoryInhibitorinhibitorinhibit

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