MK-0812, inhibitor
MK-0812
Purity
98.00%
Synonyms
MK-0812; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
DMSO: Soluble
(<1mg/ refers to the product slightly soluble or insoluble)
(<1mg/ refers to the product slightly soluble or insoluble)
Formula
C24H34F3N3O3
SMILES
CC(C1(C(N2CCC3=NC=C(C(F)(F)F)C=C3C2)=O)CCC(NC4CCOCC4OC)C1)C
CAS Number
624733-88-6
Kinase Assay
Human whole blood is collected in EDTA tubes and used within 1 h of blood collection. For antagonist treated samples, blood (200uL) is pre-incubated with MK-0812 (0.1% final DMSO concentration) for 30 minutes at room temperature. After this, 20uL of FITC conjugated anti-CD14 antibody and 4uL of chemokine or buffer is added to each sample and mixed lightly. An aliquot (100uL) of the blood mixture is incubated for 10 minutes at 37 degree C immediately placed on ice and lightly fixed with 250uL of ice-cold fixative (49mL PBS, 1.0mL 4% paraformaldehyde) for 1 minutes. Red blood cells are lysed by adding 1.0mL of ice-cold lysis solution (0.15M NH4Cl2, 10mM sodium bicarbonate, and 1mM EDTA), and incubated for 20 min on ice. After complete lysis of red blood cells, 100uL of 4% para-formaldehyde is added and the samples are analyzed by flow cytometry for forward scattering measurements [1].
In Vitro
MK0812 (30mg/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, MK0812 treatment, causes a dose-dependent reduction in circulating Ly6Chi monocytes and a corresponding elevation in the CCR2 ligand CCL2 [2].
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Related Product Information for MK-0812, inhibitor
MK-0812 is an effective and specific CCR2 antagonist.
Product Categories/Family for MK-0812, inhibitor
References
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.
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.
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.
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.
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.
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.
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.
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Product Notes
The MK-0812 (Catalog #AAA5764437) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "MK-0812, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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