SML3924
INCB3344
≥98% (HPLC)
Synonym(s):
INCB-3344, INCB 3344, trans-N-(2-{1-[4-(Benzo[d][1,3]dioxol-5-yl)-4-hydroxycyclohexyl]-4-ethoxypyrrolidin-3-ylamino}-2-oxoethyl)-3-(trifluoromethyl)benzamide
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About This Item
Empirical Formula (Hill Notation):
C29H34F3N3O6
CAS Number:
Molecular Weight:
577.59
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
Orally active, potent and selective CCR2 antagonist in vitro and in vivo.
INCB3344 is an orally active, potent and selective CCR2 antagonist (human/mouse/rat/cynomolgus IC50 = 5.1/9.5/7.3/16 nM by competitive binding assays, IC50 = 3.8/7.8/2.7/6.2 nM by chemotaxis assays) with >100-fold selectivity over other homologous chemokine receptors. INCB3344 shows in vivo efficacy in a murine EAE model (thioglycolate-induced peritonitis in mice; 30-100 mg/kg bid. p.o. against peritoneal macrophage influx) and a rat adjuvant arthritis model (100 mg/kg bid. p.o. against adjuvant-induced macrophages infiltration of the joint).
INCB3344 is an orally active, potent and selective CCR2 antagonist (human/mouse/rat/cynomolgus IC50 = 5.1/9.5/7.3/16 nM by competitive binding assays, IC50 = 3.8/7.8/2.7/6.2 nM by chemotaxis assays) with >100-fold selectivity over other homologous chemokine receptors. INCB3344 shows in vivo efficacy in a murine EAE model (thioglycolate-induced peritonitis in mice; 30-100 mg/kg bid. p.o. against peritoneal macrophage influx) and a rat adjuvant arthritis model (100 mg/kg bid. p.o. against adjuvant-induced macrophages infiltration of the joint).
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2
Bioorganic & Medicinal Chemistry Letters, 20(24), 7473-7478 (2010)
Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344
Journal of Immunology, 175(8), 5370-5378 (2005)
Pharmacological characterization of INCB3344, a small molecule antagonist of human CCR2
Biochemical and Biophysical Research Communications, 387(2), 251-255 (2009)
CCR2 receptor blockade alters blood monocyte subpopulations but does not affect atherosclerotic lesions in apoE(-/-) mice
Atherosclerosis, 208(2), 370-375 (2010)
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