您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > MK-0812
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
MK-0812
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MK-0812图片
CAS NO:624733-88-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
MK-0812 是一种有效的选择性的CCR2拮抗剂。
生物活性

MK-0812 is a potent and selectiveCCR2antagonist with low nM affinity forCCR2.

IC50& Target[1]

CCR2

 

体外研究
(In Vitro)

MK-0812 completely blocks all MCP-1 mediated response in a concentration dependent manner, with an IC50of 3.2 nM. This value is similar to the potency observed for the inhibition of125I-MCP-1 binding by MK-0812 on isolated monocytes (IC504.5 nM). In fact, the antagonist 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 IC50for MK-0812 in whole blood assays is 8 nM[1]MK0812 is a potent and selective small molecule CCR2 antagonist[2].

体内研究
(In Vivo)

MK-0812 is administered by continuous i.v. infusion to maintain a constant level of the drug in blood[1]. Administration of MK0812 at 30 mg/kg, p.o. reduces the frequency of Ly6G-Ly6Chimonocytes in the peripheral blood, while no impact on circulating Ly6G+Ly6C+neutrophil frequency is observed. In addition, MK0812 treatment causes a dose-dependent reduction in circulating Ly6Chimonocytes and a corresponding elevation in the CCR2 ligand CCL2[2].

Clinical Trial
分子量

469.54

性状

Solid

Formula

C24H34F3N3O3

CAS 号

624733-88-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month