C5aR1 antagonist 1_product_DataBase

Bioactivity	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].
Invitro	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. 0 --> C5aR1 antagonist 1 相关抗体:
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
CAS	2365325-67-1
Formula	C28H27F4N3O
Molar Mass	497.53
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Hubler, F., D. Renneberg, et al. "Discovery and Characterization of a New Class of C5aR1 Antagonists Showing In Vivo Activity." Journal of Medicinal Chemistry. 2024 March 04.

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