MK-0812 MedChemExpress (MCE)

Product Name	1,5-anhydro-2,3-dideoxy-3-(((1r,3s)-3-((7,8-dihydro-3-(trifluoromethyl)-1,6-naphthyridin-6(5h)-yl)carbonyl)-3-(1-methylethyl)cyclopentyl)amino)-4-o-methyl-d-erythro-pentitol
Synonyms	CS-206 mk 0812 MK-0812 MK0812(BASE) MK0812,MK-0812 1,5-Anhydro-2,3-dideoxy-3-[[(1R,3S)-3-[[7,8-dihydro-3-(trifluoromethyl)-1,6-naphthyridin-6(5H)-yl]carbonyl]-3-(1-methylethyl)cyclopentyl]am Synonyms CS-206 mk 0812 MK-0812 MK0812(BASE) MK0812,MK-0812 1,5-Anhydro-2,3-dideoxy-3-[[(1R,3S)-3-[[7,8-dihydro-3-(trifluoromethyl)-1,6-naphthyridin-6(5H)-yl]carbonyl]-3-(1-methylethyl)cyclopentyl]am [(1S,3R)-3-[[(3S,4S)-3-methoxyoxan-4-yl]amino]-1-propan-2-ylcyclopentyl]-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridin-6-yl]methanone 1,5-anhydro-2,3-dideoxy-3-(((1r,3s)-3-((7,8-dihydro-3-(trifluoromethyl)-1,6-naphthyridin-6(5h)-yl)carbonyl)-3-(1-methylethyl)cyclopentyl)amino)-4-o-methyl-d-erythro-pentitol 1,5-Anhydro-2,3-dideoxy-3-[[(1R,3S)-3-[[7,8-dihydro-3-(trifluoromethyl)-1,6-naphthyridin-6(5H)-yl]carbonyl]-3-(1-methylethyl)cyclopentyl]amino]-4-O-methyl-D-erythro-pentitol D-erythro-Pentitol, 1,5-anhydro-2,3-dideoxy-3-[[(1R,3S)-3-[[7,8-dihydro-3-(trifluoromethyl)-1,6-naphthyridin-6(5H)-yl]carbonyl]-3-(1-methylethyl)cyclopentyl]amino]-4-O-methyl-
CAS	624733-88-6
EINECS
Chemical Formula	C24H34F3N3O3
Molecular Weight	469.54
inchi
Package	5 mg;10 mg
Price	Email to quote
Descriptions	MK-0812 MK-0812 MedChemExpress (MCE) HY-50669 624733-88-6 98.01% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions MK-0812 MK-0812 MedChemExpress (MCE) HY-50669 624733-88-6 98.01% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. MK-0812 is a potent and selective CCR2 antagonist with low nM affinity for CCR2. 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, 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 IC50 for MK-0812 in whole blood assays is 8 nM[1] MK0812 is a potent and selective small molecule CCR2 antagonist[2]. 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-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]. Mice[2] Female BALB/c mice are used between 8 and 10 weeks of age. SCH563705 or MK0812 are administered in a 0.4% MC solution by 30 mg/kg oral gavage (p.o.). Two hours later, the frequency of CD11b+Ly6G-Ly6Chi monocytes and CD11b+Ly6G+Ly6C+ neutrophils is determined by flow cytometry. Human whole blood is collected in EDTA tubes and used within 1 h of blood collection. For antagonist treated samples, blood (200 µL) is pre-incubated with MK-0812 (0.1% final DMSO concentration) for 30 min at room temperature. After which, 20 µL of FITC conjugated anti-CD14 antibody and 4 µL of chemokine or buffer is added to each sample and mixed lightly. An aliquot (100 µL) of the blood mixture is incubated for 10 min at 37°C, immediately placed on ice and lightly fixed with 250 µL of ice cold fixative (49 mL PBS, 1.0 mL 4% para-formaldehyde) for 1 min. Red blood cells are lysed by adding 1.0 mL of ice cold lysis solution (0.15 M NH4Cl2, 10 mM sodium bicarbonate, and 1 mM EDTA), and incubated for 20 min on ice. After complete lysis of red blood cells, 100 µL of 4% para-formaldehyde is added and the samples are analyzed by flow cytometry for forward scatter measurements[1]. CCR2 \| \| \| \| \| \| \| \| \| \| [1]. 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. [Content Brief] [2]. 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. [Content Brief]
Last Update	2025-04-01 14:45:47

MedChemExpress (MCE) also provides

Thalidomide-4-O-C2-NH2

Category: Signaling Pathways
CAS: 2341840-99-9
Last Update: 2025-04-01 14:45:47

PPARα-MO-1

Category: Signaling Pathways
CAS: 810677-36-2
Last Update: 2025-04-01 14:45:47

Netupitant N-oxide

Category: Signaling Pathways
CAS: 910808-11-6
Last Update: 2025-04-01 14:45:47

TS-011

Category: Signaling Pathways
CAS: 339071-18-0
Last Update: 2025-04-01 14:45:47

SCH 530348 sulfate

Category: Signaling Pathways
CAS: 705260-08-8
Last Update: 2025-04-01 14:45:47

BAG 956

Category: Signaling Pathways
CAS: 853910-02-8
Last Update: 2025-04-01 14:45:47

YM758

Category: Signaling Pathways
CAS: 312752-85-5
Last Update: 2025-04-01 14:45:47

Thalidomide-PEG4-NH2

Category: Signaling Pathways
CAS: 2387510-82-7
Last Update: 2025-04-01 14:45:47


Supplier Name	MedChemExpress (MCE)
Contact	sales
Tel	609-228-6898
Mobile	609-228-6898
QQ
Email	sales@medchemexpress.com; tech@medchemexpress.com
Website	https://www.medchemexpress.com/
Wechat

Request for quotation

Supplier Contact