An antagonist of CCR5

TAK-779 – 5 mg

Brand:
Cayman
CAS:
229005-80-5
Storage:
-20
UN-No:
Non-Hazardous - /

TAK-779 is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).{48138,48139} It inhibits CCR5 and CXCR3 (IC50s = 236 and 369 nM, respectively, for mouse recombinant receptors expressed in 2B4 T cells) and CCR5 and CCR2b (IC50s = 1.4 and 27 nM, respectively, for human recombinant receptors expressed in CHO cells). TAK-779 inhibits the replication of clinical isolates of R5, but not X4, HIV-1 in human peripheral blood mononuclear cells (PBMCs; EC50s = 1.6-3.5 and >20,000 nM, respectively).{48138} TAK-779 (250 mg/animal per day) inhibits ovalbumin-induced increases in CCR5, CXCR3, IFN-γ, and TNF-α expression in mouse lung, as well as the number of total cells, lymphocytes, and eosinophils in bronchoalveolar lavage fluid (BALF), in a mouse model of asthma.{48140} It also increases intestinal allograft survival in a rat model of small intestine transplantation when administered at a dose of 10 mg/kg per day.{48141}  

 

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SKU: 26744 - 5 mg Category:

Description

An antagonist of CCR5, CCR2b, and CXCR3; inhibits CCR5 and CXCR3 (IC50s = 236 and 369 nM, respectively) and CCR5 and CCR2b (IC50s = 1.4 and 27 nM, respectively); inhibits the replication of clinical isolates of R5, but not X4, HIV-1 in human PBMCs (EC50s = 1.6-3.5 and >20,000 nM, respectively); inhibits ovalbumin-induced increases in CCR5, CXCR3, IFN-γ, and TNF-α expression in mouse lung, as well as the number of total cells, lymphocytes, and eosinophils in BALF, in a mouse model of asthma at 250 mg per animal per day; increases intestinal allograft survival in a rat model of small intestine transplantation at 10 mg/kg per day

Formal name: N-[[4-[[[6,7-dihydro-2-(4-methylphenyl)-5H-benzocyclohepten-8-yl]carbonyl]amino]phenyl]methyl]tetrahydro-N,N-dimethyl-2H-pyran-4-aminium, monochloride

Synonyms: 

Molecular weight: 531.1

CAS: 229005-80-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Antivirals|CCR5 Receptor Antagonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Immunology & Inflammation|Pulmonary Diseases|Asthma||Research Area|Infectious Disease|Viral Diseases|HIV & AIDS

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