| Identification | Back Directory | [Name]
INCB3344 | [CAS]
1262238-11-8 | [Synonyms]
INCB 3344;INCB-3344
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
Benzamide, N-[2-[[(3R,4R)-1-[trans-4-(1,3-benzodioxol-5-yl)-4-hydroxycyclohexyl]-4-ethoxy-3-pyrrolidinyl]amino]-2-oxoethyl]-3-(trifluoromethyl)-, rel- | [Molecular Formula]
C29H34F3N3O6 | [MDL Number]
MFCD25977164 | [MOL File]
1262238-11-8.mol | [Molecular Weight]
577.59 |
| Chemical Properties | Back Directory | [Boiling point ]
736.3±60.0 °C(Predicted) | [density ]
1.38±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≥25.9 mg/mL in DMSO; insoluble in H2O; ≥89.8 mg/mL in EtOH | [form ]
solid | [pka]
12.94±0.46(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Description]
INCB 3344 is an antagonist of chemokine (C-C motif) receptor 2 (CCR2; IC50 = 10 nM in WEHI-274 murine monocytes). It is selective for CCR2 over a panel of G protein-coupled receptors, including CCR1 and CCR5, with IC50s values greater than 1 μM. 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. 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. | [References]
[1]. brodmerkel c m, huber r, covington m, et al. discovery and pharmacological characterization of a novel rodent-active ccr2 antagonist, incb3344[j]. the journal of immunology, 2005, 175(8): 5370-5378. |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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