Avacopan,1346623-17-3

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Avacopan

CAS No. : 1346623-17-3

MCE 国际站：Avacopan

产品活性：Avacopan (CCX168) 是高效，选择性，有口服活性的补体 5a 受体 (C5aR) 抑制剂，IC₅₀ 值为0.1 nM。

研究领域：Immunology/Inflammation

作用靶点：Complement System

In Vitro: CCX168 displaces [¹²⁵I]-C5a binding to C5aR on a human myeloid cell line (U937) with a potency (IC₅₀) of 0.1 nM. CCX168 inhibits C5a-mediated chemotaxis of U937 cells with a potency (the concentration of CCX168 that produces a 2-fold right-shift in C5a activity) of 0.2 nM. CCX168 competitively and selectively blocked C5a-induced calcium mobilization in purified human neutrophils, with an IC₅₀ value of 0.2 nM. CCX168 inhibited C5a-induced release of reactive-oxygen species from isolated neutrophils, and is able to completely block respiratory burst in these neutrophils.

In Vivo: CCX168 is shown to be well tolerated across a broad dose range (1 to 100 mg) and it showed dose-dependent pharmacokinetics. An oral dose of 30 mg CCX168 given twice daily blocked the C5a-induced upregulation of CD11b in circulating neutrophils by 94% or greater throughout the entire day, demonstrating essentially complete target coverage. In mice dosed orally with 0.03 mg/kg of CCX168, the resulting plasma CCX168 concentration of 15 nM (8.7 ng/mL) reduces the drop in circulating leukocytes from 53% to 25%. In mice administered 0.3 mg/kg of CCX168, the resulting plasma CCX168 concentration of 75 nM (44 ng/mL) reduces the drop in circulating leukocytes from 53% to only 10% relative to baseline (p<0.05 for CCX168 vs. vehicle control). Oral doses of CCX168 of either 3 or 30 mg/kg completely blocks C5a-induced leukopenia in hC5aR knock-in mice. Oral CCX168, 30 mg/kg daily, reduces the severity of anti-MPO NCGN in hC5aR mice. Glomerular crescents are reduced from 30.4% to 3.3% with CCX168. Urine hematuria, proteinuria, and leukocyturia are reduced in mice receiving CCX168, 30 mg/kg per day. The protection by CCX168 results in reduced crescents and necrosis.

相关产品：Dexamethasone  |  Cyclosporin A  |  SB290157 trifluoroacetate  |  PMX 205 Trifluoroacetate  |  Danicopan  |  EG00229  |  Leukadherin-1  |  Compstatin  |  LNP023  |  ATWLPPR Peptide TFA  |  PMX-53  |  W-54011  |  BCX 1470 methanesulfonate  |  AMY-101 TFA  |  C3a (70-77) TFA  |  Complement C5-IN-1  |  EG01377 dihydrochloride  |  TLQP-21 TFA

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪制药及生命科学研究进展，为您提供全球活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。