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。

MK-0812 Succinate

CAS No. : 851916-42-2

MCE 站：MK-0812 Succinate

产品活性：MK-0812 Succinate 是一种有效的选择性 CCR2 拮抗剂。

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

作用靶点：CCR

In Vitro: MK-0812 is a potent ａnd selective CCR2 antagonist. MK-0812 completely blocks all MCP-1 mediated response in a concentration dependent manner, with an IC₅₀ of 3.2 nM. This value is similar to the potency observed for the inhibition of ¹²⁵I-MCP-1 binding by MK-0812 on isolated monocytes (IC₅₀ 4.5 nM). In fact, MK-0812 not only completely blocks the shape change response to exogenous MCP-1, but also results in a monocyte forward scatter measurement below unstimulated or basal levels. The addition of MK-0812 to rhesus blood also inhibits MCP-1 induced monocyte shape change. The IC₅₀ for MK-0812 in whole blood assays is 8 nM

In Vivo: MK-0812 (30 mg/kg, p.o.) reduces the frequency of Ly6G^-Ly6C^hi monocytes in the peripheral blood, while no impact on circulating Ly6G⁺Ly6C⁺ neutrophil frequency is observed. In addition, MK-0812 treatment causes a dose-dependent reduction in circulating Ly6C^hi monocytes ａnd a corresponding elevation in the CCR2 ligand CCL2. MK-0812 is administered by continuous i.v. infusion to maintain a constant level of the drug in blood.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Immunology/Inflammation Compound Library  |  Clinical Compound Library  |  Small Molecule Immuno-Oncology Compound Library  |  Drug Repurposing Compound Library  |  Endocrinology 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  |  INCB 3284  |  CCR2 antagonist 4 hydrochloride  |  J-113863  |  DAPTA  |  Vicriviroc maleate  |  K777  |  LMD-009  |  SB297006  |  ZK756326 dihydrochloride  |  CCR2 antagonist 3  |  AZD2423  |  CCR2 antagonist 1

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。