A potent CCR2 antagonist (IC50 = 5 nM for human CCR2); not efficacious in a mouse model of arthritis or in clinical trials for rheumatoid arthritis and multiple sclerosis

MK-0812 – 5 mg

Brand:
Cayman
CAS:
624733-88-6
Storage:
-20
UN-No:
Non-Hazardous - /

MK-0812 is a potent C-C chemokine receptor type 2 (CCR2) antagonist (IC50 = 5 nM for human CCR2).{34341} In a mouse model of antibody-induced arthritis, MK-0812 did not affect disease severity.{34340} Clinical trials for the use of MK-0812 for rheumatoid arthritis and multiple sclerosis were terminated early due to a lack of efficacy.{34342,34339}  

 

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Description

A potent CCR2 antagonist (IC50 = 5 nM for human CCR2); not efficacious in a mouse model of arthritis or in clinical trials for rheumatoid arthritis and multiple sclerosis

Formal 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: 

Molecular weight: 469.5

CAS: 624733-88-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Innate Immunity

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