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| | INCB3344 Basic information |
| Product Name: | INCB3344 | | Synonyms: | 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;INCB 3344;INCB-3344;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-;CC chemokine receptor,INCB3344,CCR,Inhibitor,inhibit,INCB-3344,INCB 3344 | | CAS: | 1262238-11-8 | | MF: | C29H34F3N3O6 | | MW: | 577.59 | | EINECS: | | | Product Categories: | API | | Mol File: | 1262238-11-8.mol |  |
| | INCB3344 Chemical Properties |
| 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 |
| | INCB3344 Usage And Synthesis |
| 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. |
| | INCB3344 Preparation Products And Raw materials |
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