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。

INCB 3284

CAS No. : 887401-92-5

MCE 站：INCB 3284

产品活性：INCB 3284 是一种有效的，选择性的人 CCR2 拮抗剂，能够抑制单核细胞趋化蛋白 1 与 hCCR2 结合，IC₅₀ 值为 3.7 nM。INCB 3284 可用于急性肝功能衰竭的研究。

研究领域：GPCR/G Protein  |  Immunology/Inflammation

作用靶点：CCR

In Vitro: INCB 3284 is a pentent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC₅₀ of 3.7 nM. INCB 3284 also causes an IC₅₀ of 4.7 nM in antagonism of chemotaxis activity, an IC₅₀ of 84 μM in inhibition of the hERG potassium current. However, INCB 3284 has no effec on CCR1, CCR3, CCR5, CXCR3, and CXCR5, or additional GPCRs at a concentration of 1 μM. Moreover, INCB 3284 potently inhibits CCR2-mediated signaling events such as intracellular calcium mobilization and ERK phosphorylation with IC₅₀ values of 6 and 2.6 nM, respectively.

In Vivo: INCB 3284 (1 mg/kg/day, ip) reduces liver damage, and decreases microglia activation in AOM-treated mice via inhibition on CCR2. INCB 3284 also significantly reduces the pERK1/2 to tERK1/2 ratio, as well as G-protein signaling pathway activity and proinflammatory cytokine production in cortex lysates from mice administed with azoxymethane.

相关产品：Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Immunology/Inflammation Compound Library  |  Small Molecule Immuno-Oncology Compound Library  |  Endocrinology Compound Library  |  Orally Active Compound Library  |  Pirfenidone  |  Maraviroc  |  RS 504393  |  INCB3344  |  PF-4136309  |  Bindarit  |  BX471  |  TAK-779  |  RS102895 hydrochloride  |  AZ084  |  CCR6 inhibitor 1  |  CCR2-RA-[R]  |  7,4'-Dihydroxyflavone  |  TAK-220  |  CCR2 antagonist 4 hydrochloride  |  J-113863  |  DAPTA  |  Vicriviroc maleate  |  K777  |  LMD-009  |  SB297006  |  ZK756326 dihydrochloride  |  CCR2 antagonist 3  |  AZD2423  |  CCR2 antagonist 1  |  YM022

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*新*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 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。