| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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INCB3284 (INCB-3284) is a novel, potent and orally bioavailable CCR2 antagonist with the potential to be used for acute liver failure. Acts by inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM.
| 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].
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| 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].
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| References |
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| Additional Infomation |
INCB3284 is a CCR2 antagonist for Inflammation-driven Diseases.
Drug Indication Investigated for use/treatment in inflammatory disorders (unspecified). |
| 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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