貨號	規格	價格	上海	北京	武漢	南京	購買數量
S86755-5mg	99.3%	￥1490.00 S86755-5mg ￥1490.00 現貨	11 0 >10	-	-	-
S86755-10mg	99.3%	￥2750.00 S86755-10mg ￥2750.00 現貨	14 >10	-	-	-

產品介紹

MK-0812 Succinate is a potent and selective CCR2 antagonist with high affinity at CCR2

產品描述：

MK-0812 Succinate is a potent and selective CCR2 antagonist with high affinity at CCR2

靶點：

CCR2;CCR

體外研究：

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

體內研究：

MK-0812 (30 mg/kg, p.o.) reduces the frequency of Ly6G-Ly6Chi?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 Ly6Chi?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.

參考文獻：

1. Min SH, et al. Pharmacological targeting reveals distinct roles for CXCR2/CXCR1 and CCR2 in a mouse model of arthritis.Biochem Biophys Res Commun. 2010 Jan 1;391(1):1080-6. 2. Wisniewski T, et al. Assessment of chemokine receptor function on monocytes in whole blood: In vitro and ex vivo evaluations of a CCR2 antagonist.J Immunol Methods. 2010 Jan 31;352(1-2):101-10.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.702 ml	8.509 ml	17.018 ml
5 mM	0.34 ml	1.702 ml	3.404 ml
10 mM	0.17 ml	0.851 ml	1.702 ml
50 mM	0.034 ml	0.17 ml	0.34 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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MK-0812 (Succinate)