- INCB 3284 dimesylate
- INCB3344
- INCB8761(PF-4136309)
- RS 504393
| MK-0812antagonist of chemokine receptor CCR-2 |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
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| Cas No. | 624733-88-6 | SDF | Download SDF |
| Synonyms | MK 0812; MK0812 | ||
| 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 | ||
| Canonical SMILES | CC(C1(C(N2CCC3=NC=C(C(F)(F)F)C=C3C2)=O)CCC(NC4CCOCC4OC)C1)C | ||
| Formula | C24H34F3N3O3 | M.Wt | 469.54 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
MK-0812 is an antagonist of chemokine receptor CCR-2 [1].C-C chemokine receptor type 2 (CCR-2) is a chemokine receptor expressing on monocytes and macrophages and plays a critical and apparently non-redundant role in orchestrating the trafficking of monocytes to tissues [1].In human whole blood, MK-0812 completely blocked all MCP-1 mediated response with IC50 value of 3.2 nM in a concentration dependent way, which is similar to the inhibition of 125I-MCP-1 binding by MK-0812 on isolated monocytes (IC50 4.5 nM). Also, MK-0812 resulted in a monocyte forward scatter measurement below unstimulated or basal levels. In rhesus whole blood, MK-0812 inhibited monocyte shape change with IC50 value of 8 nM. MK-0812 inhibited monocyte recruitment in a dose-dependent way which related with the inhibition of MCP-1 induced monocyte shape change [1].In naive BALB/c mice, MK-0812 (30 mg/kg) reduced the frequency of Ly6G-Ly6Chi monocytes in the peripheral blood. In addition, MK-0812 reduced circulating Ly6Chi monocytes and increased the CCR2 ligand CCL2 in a dose-dependent way [2].References:[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.
