| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
CCR2
INCB3344 R-isomer targets CCR2, a G protein-coupled receptor (GPCR) that binds monocyte chemoattractant protein-1 (MCP-1/CCL2). By blocking CCR2, the compound inhibits the recruitment of monocytes and macrophages to sites of inflammation, thereby modulating immune responses. The R-isomer exhibits potent binding antagonism with IC50 values of 5.1 nM for human CCR2 and 9.5 nM for mouse CCR2. |
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| ln Vitro |
INCB3344 R-isomer demonstrates potent CCR2 antagonism in cell-free binding assays, with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2). The R-isomer also shows excellent selectivity over other chemokine receptors, with no significant activity against CCR1, CCR3, CCR4, CCR5, or CCR8 at concentrations up to 10 microM.
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| ln Vivo |
In cellular chemotaxis assays, INCB3344 R-isomer inhibits MCP-1-induced migration of human monocytes and mouse splenocytes with IC50 values of 3.8 nM (hCCR2) and 7.8 nM (mCCR2). The compound also reduces calcium flux and ERK phosphorylation in response to MCP-1 stimulation, confirming functional antagonism of the CCR2 signaling pathway.
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| Enzyme Assay |
The CCR2 binding affinity of INCB3344 R-isomer is measured using a cell-free radioligand displacement assay. Membranes from CHO cells expressing human CCR2 are incubated with 125I-labeled MCP-1 in the presence of increasing concentrations of the test compound. Bound radioactivity is measured after filtration, and IC50 values are calculated from displacement curves. The assay is performed in duplicate with appropriate controls.
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| Cell Assay |
For chemotaxis inhibition assays, human THP-1 monocytes or primary human monocytes are loaded into the upper chamber of a transwell plate. MCP-1 is added to the lower chamber as a chemoattractant. Cells are pre-incubated with INCB3344 R-isomer (0.1-1000 nM) for 30 minutes. After incubation (2-4 hours), migrated cells are quantified by fluorescence or manual counting. IC50 values are calculated from dose-response curves.
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| Animal Protocol |
In a mouse model of thioglycollate-induced peritonitis, INCB3344 R-isomer is administered orally (10-30 mg/kg) 1 hour prior to thioglycollate injection. Peritoneal lavage is performed 4 hours later, and the number of infiltrated monocytes/macrophages is counted. The compound significantly reduces cell infiltration at 30 mg/kg, demonstrating in vivo CCR2 antagonism. Other models include collagen-induced arthritis (CIA) and experimental autoimmune encephalomyelitis (EAE).
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| ADME/Pharmacokinetics |
INCB3344 R-isomer is orally bioavailable with good absorption and systemic exposure. In rats, the compound achieves peak plasma concentrations within 1-2 hours after oral administration. The half-life is approximately 3-5 hours, allowing once- or twice-daily dosing in animal studies. Plasma protein binding is moderate, and the compound shows good tissue distribution.
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| Toxicity/Toxicokinetics |
In preclinical toxicity studies, INCB3344 R-isomer is well-tolerated at doses up to 100 mg/kg in rodents. No significant adverse effects on body weight, food consumption, or clinical chemistry parameters have been observed. Organ histopathology reveals no treatment-related abnormalities. Longer-term toxicity studies are required for further development.
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| References | |
| Additional Infomation |
INCB3344 R-isomer is a research compound used primarily for investigating CCR2 biology and validating the receptor as a therapeutic target. It has not been approved for clinical use. The R-isomer is the preferred form for pharmacological studies as it retains higher potency compared to the S-isomer or racemic mixture. The compound is supplied as a powder for reconstitution.
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| Molecular Formula |
C29H34F3N3O6
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| Molecular Weight |
577.59
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| Related CAS # |
INCB3344;1262238-11-8
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| Appearance |
Light yellow to yellow solid powder
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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 :≥ 106.5 mg/mL (~184.39 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7313 mL | 8.6567 mL | 17.3133 mL | |
| 5 mM | 0.3463 mL | 1.7313 mL | 3.4627 mL | |
| 10 mM | 0.1731 mL | 0.8657 mL | 1.7313 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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