MK-0812
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
MK-0812是趋化因子受体CCR2拮抗剂[1]。
CC趋化因子受体2（CCR-2）是一类由单核细胞和巨噬细胞表达的趋化因子受体，在协调单核细胞转移至组织中起着关键作用[1]。
在人全血中，MK-0812以剂量依赖的方式完全阻断MCP-1介导的应答，IC50值为3.2 nM。在分离的单核细胞中，MK-0812也呈浓度依赖性地抑制125I-MCP-1结合（IC50 = 4.5 nM）。此外，MK-0812导致单核细胞的前向散射光测量值低于未刺激的或基线的水平。在恒河猴全血中，MK-0812抑制单核细胞形态变化，其IC50值为8 nM。MK-0812剂量依赖性地抑制单核细胞募集，这与MK-0812对MCP-1诱导的单核细胞形态变化的抑制相关[1]。
在初始BALB/c小鼠中，MK-0812（30 mg/kg）减少外周血中的Ly6G-Ly6Chi单核细胞。此外，MK-0812减少循环的Ly6Chi单核细胞，并剂量依赖性地增加CCR2的配体CCL2[2]。
参考文献：
[1]. Wisniewski T, Bayne E, Flanagan J, 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, 352(1-2): 101-110.
[2]. Min SH, Wang Y, Gonsiorek W, et al. Pharmacological targeting reveals distinct roles for CXCR2/CXCR1 and CCR2 in a mouse model of arthritis. Biochem Biophys Res Commun, 2010, 391(1): 1080-1086.
| Storage | Store at -20°C |
| M.Wt | 469.54 |
| Cas No. | 624733-88-6 |
| Formula | C24H34F3N3O3 |
| Synonyms | MK 0812; MK0812 |
| Solubility | Soluble in DMSO |
| Chemical Name | (1-isopropyl-3-((3-methoxytetrahydro-2H-pyran-4-yl)amino)cyclopentyl)(3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl)methanone |
| SDF | Download SDF |
| Canonical SMILES | CC(C1(C(N2CCC3=NC=C(C(F)(F)F)C=C3C2)=O)CCC(NC4CCOCC4OC)C1)C |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
