INCB 3344

INCB 3344 is an antagonist of chemokine (C-C motif) receptor 2 (CCR2; IC50 = 10 nM in WEHI-274 murine monocytes).1 It is selective for CCR2 over a panel of G protein-coupled receptors, including CCR1 and CCR5, with IC50s values greater than 1 µM.2 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.1 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.2WARNING This product is not for human or veterinary use.

An antagonist of CCR2

577.6

≥95%

Biochemicals/Receptor Pharmacology/Antagonists

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

CCO[C@@H]1[C@@H](NC(CNC(C2=CC=CC(C(F)(F)F)=C2)=O)=O)CN([C@]3([H])CC[C@@](C4=CC=C(OCO5)C5=C4)(O)CC3)C

C29H34F3N3O6

1262238-11-8

≥ 4 years

DMSO: soluble