| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
INCB 3284 targets the CCR2 receptor, a G-protein coupled receptor for monocyte chemoattractant protein-1 (MCP-1). It potently inhibits the interaction of MCP-1 with hCCR2, with an IC50 of 3.7 nM. By blocking this interaction, it disrupts the chemotaxis of monocytes and other immune cells, thereby modulating inflammatory responses.
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| ln Vitro |
INCB 3284 is a powerful, specific, and highly bioavailable human CCR2 antagonist that prevents monocyte chemoattractant protein-1 from binding to hCCR2 with an IC50 of 3.7 nM. INCB 3284 has an IC50 of 4.7 nM for antagonizing chemotactic activity and an IC50 of 84 μM for inhibiting hERG potassium currents. However, INCB 3284 at a concentration of 1 μM had no effect on CCR1, CCR3, CCR5, CXCR3, and CXCR5 or other GPCRs. In addition, INCB 3284 effectively inhibits CCR2-mediated signaling events, such as intracellular induction and ERK phosphorylation, with IC50 values of 6 and 2.6 nM, respectively [1].
In vitro, INCB 3284 demonstrates potent antagonist activity. It inhibits MCP-1 binding to hCCR2 with an IC50 of 3.7 nM. This activity is confirmed in functional assays where it blocks CCR2-mediated signaling, such as calcium mobilization and chemotaxis. Its selectivity for CCR2 over other chemokine receptors has been demonstrated. |
| ln Vivo |
By blocking CCR2, INCB 3284 (1 mg/kg/day, i.p.) lessens liver damage and lowers small cell activation in rats treated with AOM. Additionally, INCB 3284 markedly decreased proinflammatory cytokine production in the brain, G protein signal amplifier activity, and ischemia of pERK1/2 and tERK1/2 [2].
In vivo, INCB 3284 has been studied for its potential therapeutic effects. It has been investigated for the treatment of hemorrhagic shock and acute liver failure. By blocking CCR2, it can reduce the infiltration of inflammatory cells into tissues, thereby attenuating inflammation and tissue damage. Its oral bioavailability makes it suitable for in vivo studies. |
| Enzyme Assay |
The in vitro receptor binding assay for INCB 3284 involves competitive binding studies using membranes from cells expressing hCCR2. The compound is incubated with a radiolabeled ligand, such as [125I]-MCP-1, in the presence of varying concentrations. The amount of radioligand displaced is measured to determine the binding affinity (Ki) and the IC50 for inhibition.
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| Cell Assay |
In vitro cell-based functional assays for INCB 3284 utilize cells expressing the CCR2 receptor, such as monocytes or transfected cell lines. Cells are loaded with a calcium-sensitive dye and stimulated with a CCR2 agonist like MCP-1. The antagonist's ability to inhibit the increase in intracellular calcium is measured, and the IC50 is calculated from the concentration-response curve. Chemotaxis assays can also be performed.
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| Animal Protocol |
In vivo animal experiments for INCB 3284 have been performed in models of hemorrhagic shock and acute liver failure. In these models, the compound is administered orally or intraperitoneally. Endpoints such as survival rate, tissue damage (histopathology), and inflammatory cytokine levels (ELISA) are assessed to evaluate its protective effects.
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| ADME/Pharmacokinetics |
INCB 3284 has a molecular formula of C26H31F3N4O4 and a molecular weight of 520.54 g/mol. It is a solid compound that is soluble in DMSO. It is orally bioavailable. It is typically stored as a powder at -20°C for long-term stability. Its stability is maintained under recommended storage conditions. For in vivo studies, it is formulated in suitable vehicles.
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| Toxicity/Toxicokinetics |
Toxicological data for INCB 3284 are limited, as it is a research compound. It is not intended for human use. Comprehensive toxicity studies have not been reported. Standard safety precautions for handling chemical reagents should be followed. Its potent CCR2 antagonism suggests it could have significant immunomodulatory effects.
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| References |
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| Additional Infomation |
INCB3284 is a CCR2 antagonist used to treat inflammatory diseases.
Drug Indications It has been investigated for the treatment of inflammatory diseases (not specified). INCB 3284 is a research compound with no clinical approval. It is a valuable tool for studying CCR2 biology and the role of the MCP-1/CCR2 axis in inflammation and disease. It is used in drug discovery programs to explore the therapeutic potential of CCR2 antagonism for the treatment of autoimmune diseases, inflammatory disorders, and other conditions. |
| Molecular Formula |
C₂₆H₃₁F₃N₄O₄
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|---|---|
| Molecular Weight |
520.54
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| Exact Mass |
520.23
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| CAS # |
887401-92-5
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| Related CAS # |
INCB 3284 dimesylate;887401-93-6
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| PubChem CID |
11527661
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| Appearance |
Off-white to yellow solid powder
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| LogP |
3.579
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
37
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| Complexity |
790
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| Defined Atom Stereocenter Count |
1
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| SMILES |
COC1=NC=C(C=C1)C2(CCC(CC2)N3CC[C@H](C3)NC(=O)CNC(=O)C4=CC(=CC=C4)C(F)(F)F)O
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| InChi Key |
NXZNYBUBXWWKCP-DNRQZRRGSA-N
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| InChi Code |
InChI=1S/C26H31F3N4O4/c1-37-23-6-5-19(14-30-23)25(36)10-7-21(8-11-25)33-12-9-20(16-33)32-22(34)15-31-24(35)17-3-2-4-18(13-17)26(27,28)29/h2-6,13-14,20-21,36H,7-12,15-16H2,1H3,(H,31,35)(H,32,34)/t20-,21-,25-/m1/s1
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| Chemical Name |
Benzamide, N-(2-(((3R)-1-(trans-4-hydroxy-4-(6-methoxy-3-pyridinyl)cyclohexyl)-3-pyrrolidinyl)amino)-2-oxoethyl)-3-(trifluoromethyl)-
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| Synonyms |
INCB 3284 INCB3284 INCB-3284
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 83.3 mg/mL (~160.03 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.80 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.80 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9211 mL | 9.6054 mL | 19.2108 mL | |
| 5 mM | 0.3842 mL | 1.9211 mL | 3.8422 mL | |
| 10 mM | 0.1921 mL | 0.9605 mL | 1.9211 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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