An antagonist of CCR2 (IC50 = 10 nM); selective for CCR2 over a panel of G protein-coupled receptors

INCB 3344 – 10 mg

Brand:
Cayman
CAS:
1262238-11-8
Storage:
-20
UN-No:
Non-Hazardous - /

INCB 3344 is an antagonist of chemokine (C-C motif) receptor 2 (CCR2; IC50 = 10 nM in WEHI-274 murine monocytes).{48545} It is selective for CCR2 over a panel of G protein-coupled receptors, including CCR1 and CCR5, with IC50s values greater than 1 µM.{48546} INCB 3344 inhibits chemotaxis of WEHI-274 cells induced by chemokine (C-C motif) ligand 2 (CCL2; IC50 = 10 nM) and CCL2-induced phosphorylation of ERK in WEHI-274 cells.{48545} It inhibits monocyte influx in a mouse model of peritonitis induced by thioglycolate when administered at doses of 60 and 100 mg/kg. INCB 3344 (30, 50, and 100 mg/kg twice per day) decreases the expression of CCR2 mRNA in the ear and reduces ear swelling in a mouse model of delayed-type hypersensitivity reaction. It prevents increases in or reduces macrophage levels in the spinal cord when administered at a dose of 100 mg/kg per day beginning the day of immunization or seven days following immunization, respectively, in a mouse model of experimental autoimmune encephalomyelitis (EAE). It also reduces disease incidence and severity in the same model and reduces disease severity in a rat model of adjuvant-induced arthritis. INCB 3344 reduces macrophage infiltration to the kidney and improves renal function in a mouse model of polycystic kidney disease.{48546}  

 

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Description

An antagonist of CCR2 (IC50 = 10 nM); selective for CCR2 over a panel of G protein-coupled receptors, including CCR1 and CCR5, with IC50s values >1 µM; inhibits MCP-1-induced chemotaxis of WEHI-274 cells (IC50 = 10 nM); inhibits monocyte influx in a thioglycolate-induced mouse model of peritonitis at 60 and 100 mg/kg; decreases the expression of CCR2 mRNA in the ear and reduces ear swelling in a mouse model of delayed-type hypersensitivity reaction at 30, 50, and 100 mg/kg twice per day; prevents increases in or reduces macrophage levels in the spinal cord at 100 mg/kg per day beginning the day of immunization or seven days following immunization, respectively, in a mouse model of EAE

Formal name: rel-N-[2-[[(3R,4R)-1-[trans-4-(1,3-benzodioxol-5-yl)-4-hydroxycyclohexyl]-4-ethoxy-3-pyrrolidinyl]amino]-2-oxoethyl]-3-(trifluoromethyl)-benzamide

Synonyms: 

Molecular weight: 577.6

CAS: 1262238-11-8

Purity: ≥98%

Formulation: A solid

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