INCB3344
Based on 30 publication(s) in Google Scholar
INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
For research use only. We do not sell to patients.
- Purity: 99.81%
- CAS No.: 1262238-11-8
- Formula: C29H34F3N3O6
- Molecular Weight:577.59
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) INCB3344
More- Signal Transduct Target Ther. 2025 Oct 28;10(1):357. [Abstract]
- Adv Sci (Weinh). 2024 Sep 3:e2405364. [Abstract]
- Kidney Int. 2026 Mar 13:S0085-2538(26)00162-6. [Abstract]
- J Neuroinflammation. 2021 Sep 12;18(1):196. [Abstract]
- J Am Soc Nephrol. 2018 Oct;29(10):2471-2481. [Abstract]
- EMBO Mol Med. 2015 Mar 14;7(5):547-61. [Abstract]
- Hypertension. 2012 Nov;60(5):1207-12. [Abstract]
- Diabetes. 2019 Nov;68(11):2063-2073. [Abstract]
- EMBO Rep. 2016 Dec;17(12):1738-1752. [Abstract]
- Cancer Cell Int. 2023 Oct 11;23(1):237. [Abstract]
- Acta Neuropathol Commun. 2014 Aug 23;2(1):98. [Abstract]
- Inflammopharmacology. 2018 Feb;26(1):207-215. [Abstract]
- Inflammation. 2026 Jan 15;49(1):48. [Abstract]
- Neuropharmacology. 2025 Nov 15:279:110625. [Abstract]
- Cancers (Basel). 2023 Mar 6;15(5):1620. [Abstract]
- J Neurosci. 2015 Jan 7;35(1):4-20. [Abstract]
- J Biol Chem. 2018 Jun 22;293(25):9685-9695. [Abstract]
- Chem Res Toxicol. 2025 Mar 26. [Abstract]
- Hum Vaccin Immunother. 2017 Dec 2;13(12):2872-2882. [Abstract]
- Neuroscience. 2020 Jan 15;425:29-38. [Abstract]
- Mol Pain. 2018 Jan-Dec;14:1744806917751322. [Abstract]
- Immun Inflamm Dis. 2024 Nov;12(11):e70073. [Abstract]
- Biochem Biophys Res Commun. 2022 Mar 12;596:63-70. [Abstract]
- bioRxiv. 2025 Oct 13.
- Res Sq. 2025 Sep 26.
- bioRxiv. 2025 May 21:2025.05.19.655010. [Abstract]
- bioRxiv. 2023 Aug 13.
- Patent. US20220175912A1.
- Oncotarget. 2018 Jul 13;9(76):34213-34228. [Abstract]
- University of Toronto. 2016 Nov.
Customer Validation & Images
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IHC
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
Biological Activity
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hCCR2 5.1 nM (IC50) |
mCCR2 9.5 nM (IC50) |
INCB3344 is a potent antagonist towards rat and cynomolgus CCR2 as well, displaying IC50 values of 7.3 and 16 nM in binding antagonism and 2.7 and 6.2 nM in antagonism of chemotaxis activity, respectively. INCB3344 is a selective hCCR2 antagonist, exhibiting IC50 values of more than 1 μM against a panel of >50 ion channels, transporters, chemokine receptors and other selected GPCRs. It is also a selective mCCR2 antagonist, showing IC50 values of >1 μM and >3 μM against murine CCR1 and murine CCR5, respectively, the two most homologous chemokine receptors to mCCR2[1]. Characterization of the pharmacological activity of INCB3344 is first evaluated by testing its ability to inhibit CCL2 binding to CCR2 in a whole cell binding assay using a murine monocyte cell line, WEHI-274.1 and 125I-labeled mCCL2 as a tracer. The binding IC50 of INCB3344 in this assay is determined to be 10±5 nM, and inhibition of >90% binding is observed at a concentration of 90 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1262238-11-8
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Appearance Solid
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Molecular Weight 577.59
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Formula C29H34F3N3O6
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Color White to yellow
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SMILES
CCO[C@H]1CN([C@]2([H])CC[C@@](CC2)(C3=CC4=C(OCO4)C=C3)O)C[C@@H]1NC(CNC(C5=CC(C(F)(F)F)=CC=C5)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (30)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Piezo1 activation suppresses bone marrow adipogenesis to prevent osteoporosis by inhibiting a mechanoinflammatory autocrine loop. [Abstract]2025 Oct 28;10(1):357. PMID: 41145414 -
Adv Sci (Weinh)
Nanotherapeutic Approaches of Interleukin-3 to Clear the α-Synuclein Pathology in Mouse Models of Parkinson's Disease. [Abstract]2024 Sep 3:e2405364. PMID: 39225429 -
Kidney Int
The role of C-C motif chemokine ligand 2 in the preservation of myogenic tone in the kidney microvasculature of Dahl Salt-Sensitive rats. [Abstract]2026 Mar 13:S0085-2538(26)00162-6. PMID: 41833640 -
J Neuroinflammation
Small extracellular vesicles encapsulating CCL2 from activated astrocytes induce microglial activation and neuronal apoptosis after traumatic spinal cord injury. [Abstract]2021 Sep 12;18(1):196. PMID: 34511129 -
J Am Soc Nephrol
Mcp1 Promotes Macrophage-Dependent Cyst Expansion in Autosomal Dominant Polycystic Kidney Disease. [Abstract]2018 Oct;29(10):2471-2481. PMID: 30209078 -
EMBO Mol Med
Low-dose TNF augments fracture healing in normal and osteoporotic bone by up-regulating the innate immune response. [Abstract]2015 Mar 14;7(5):547-61. PMID: 25770819 -
Hypertension
Reversal of vascular macrophage accumulation and hypertension by a CCR2 antagonist in deoxycorticosterone/salt-treated mice. [Abstract]2012 Nov;60(5):1207-12. PMID: 23033370
INCB3344 purchased from MedChemExpress. Usage Cited in: Hypertension. 2012 Nov;60(5):1207-12. [Abstract]
Effect of intervention with a CCR2 antagonist, INCB3344 (30 mg/kg per day), on Deoxycorticosterone acetate/salt-induced increases in expression of CCR2 (A), CCL2 (B), CCL7 (C), CCL8 (D), and CCL12 (E) in aortas of mice.
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Diabetes
2019 Nov;68(11):2063-2073. PMID: 31439648 -
EMBO Rep
Central CCL2 signaling onto MCH neurons mediates metabolic and behavioral adaptation to inflammation. [Abstract]2016 Dec;17(12):1738-1752. PMID: 27733491 -
Cancer Cell Int
A novel STAT3/ NFκB p50 axis regulates stromal-KDM2A to promote M2 macrophage-mediated chemoresistance in breast cancer. [Abstract]2023 Oct 11;23(1):237. PMID: 37821959 -
Acta Neuropathol Commun
Discrepancy in CCL2 and CCR2 expression in white versus grey matter hippocampal lesions of Multiple Sclerosis patients. [Abstract]2014 Aug 23;2(1):98. PMID: 25149422 -
Inflammopharmacology
Antihyperalgesic effects of ashwagandha (Withania somnifera root extract) in rat models of postoperative and neuropathic pain. [Abstract]2018 Feb;26(1):207-215. PMID: 28849547 -
Inflammation
Activation of β2-Adrenergic Receptor Alleviates Viral Myocarditis by Regulating Energy Metabolism in Monocyte-derived Macrophages via the AMPK Pathway. [Abstract]2026 Jan 15;49(1):48. PMID: 41537900 -
Neuropharmacology
Brain-invading monocytes promote seizure-associated cognitive deficits and neurodegeneration. [Abstract]2025 Nov 15:279:110625. PMID: 40769260 -
Cancers (Basel)
Cancer-Associated Fibroblasts Exposed to High-Dose Ionizing Radiation Promote M2 Polarization of Macrophages, Which Induce Radiosensitivity in Cervical Cancer. [Abstract]2023 Mar 6;15(5):1620. PMID: 36900416 -
J Neurosci
Demyelination causes adult CNS progenitors to revert to an immature state and express immune cues that support their migration. [Abstract]2015 Jan 7;35(1):4-20. PMID: 25568099 -
J Biol Chem
The prostaglandin E2 receptor EP3 controls CC-chemokine ligand 2-mediated neuropathic pain induced by mechanical nerve damage. [Abstract]2018 Jun 22;293(25):9685-9695. PMID: 29752406 -
Chem Res Toxicol
RNA Methylation and Transcriptome Analysis Reveal Key Regulatory Pathways Related to Cadmium-Induced Liver Damage. [Abstract]2025 Mar 26. PMID: 40135526 -
Hum Vaccin Immunother
Enrichment of Ly6Chi monocytes by multiple GM-CSF injections with HBV vaccine contributes to viral clearance in a HBV mouse model. [Abstract]2017 Dec 2;13(12):2872-2882. PMID: 28699816
INCB3344 purchased from MedChemExpress. Usage Cited in: Hum Vaccin Immunother. 2017 Dec 2;13(12):2872-2882. [Abstract]
Blockage of Ly6Chi monocytes abrogates HBV clearance by the 3 × GM-CSF+VACCINE. The AAV8–1.3HBV infected mice are treated with CCR2 antagonist (INCB 3344, 30 mg/kg) by intraperitoneal injection one hour before GM-CSF, repeated at day 2, 3, and 4. The CD11b+Ly6Chi monocytes are measured 12 hours after the fourth INCB 3344 administration.
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Neuroscience
CCL2-CCR2 Axis Potentiates NMDA Receptor Signaling to Aggravate Neuropathic Pain Induced by Brachial Plexus Avulsion. [Abstract]2020 Jan 15;425:29-38. PMID: 31805255 -
Mol Pain
CCR2 upregulation in DRG neurons plays a crucial role in gastric hyperalgesia associated with diabetic gastropathy. [Abstract]2018 Jan-Dec;14:1744806917751322. PMID: 29359616 -
Immun Inflamm Dis
Formoterol Reduces the Pro-Inflammatory Phenotype by Enhancing the Activity of Glutaminase in Monocyte-Derived Macrophages in the CVB3-Induced Viral Myocarditis. [Abstract]2024 Nov;12(11):e70073. PMID: 39601476 -
Biochem Biophys Res Commun
Estrogen receptor α mediated M1/M2 macrophages polarization plays a critical role in NASH of female mice. [Abstract]2022 Mar 12;596:63-70. PMID: 35114586 -
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bioRxiv
CCR2 antagonism identifies blood-borne monocytes as a target for prevention of cognitive deficits after seizures. [Abstract]2025 May 21:2025.05.19.655010. PMID: 40475612 -
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Oncotarget
Clearance of HBeAg and HBsAg of HBV in mice model by a recombinant HBV vaccine combined with GM-CSF and IFN-α as an effective therapeutic vaccine adjuvant. [Abstract]2018 Jul 13;9(76):34213-34228. PMID: 30344938
INCB3344 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Jul 13;9(76):34213-34228. [Abstract]
The use of INCB 3344 leads to significant reduction of HBsAgs.
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Solvent & Solubility
DMSO : 100 mg/mL (173.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (8.66 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (8.66 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
WEHI-274.1 cells (5×105) in RPMI 1640 (VWR) with or without various concentrations of INCB3344 in RPMI 1640 are loaded in the wells on top of an 8-μm polycarbonate filter in a 96-well-modified Boyden chamber. Beneath the filter, 30 nM mCCL2 with or without INCB3344 or media is placed in a corresponding 96-well plate. The sealed chambers are incubated for 45 min at 37°C, 5% CO2. Filters are washed, stained with Wright-Giemsa, and the number of cells that migrate toward mCCL2 in the bottom chamber counted by microscopy. The ability of INCB3344 to antagonize CCR2-mediated chemotaxis is reported as the inhibitor concentration required for IC50 values of specific migration to mCCL2. Specific migration is defined as the total migration minus the background migration. A similar assay is used to determine the impact of INCB3344 on CCR1-mediated chemotaxis of WEHI-274.1 cells, by using mouse MIP-1α as a ligand. In addition C5a, FMLP and RANTES are similarly tested in the presence of INCB3344 for migration of WEHI-274.1 cells. For the studies on the impact of INCB3344 on CCR5-mediated chemotaxis, murine T cells are used as the cell system with mouse MIP-1β as the ligand[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
In a subset of experiments, Deoxycorticosterone acetate/salt-treated mice are further randomly assigned to receive the CCR2 antagonist, INCB3344 (30 mg/kg per day; Haoyuan Chemexpress Co Ltd) or vehicle (10% DMSO/0.9% carboxymethylcellulose) via daily intraperitoneal injections commencing 10 days after induction of hypertension and continuing until the end of the 21-day treatment period. The normotensive control group for these experiments consist of sham-treated mice that receive vehicle from days 10 to 21.
Rats[4]
Adult male Sprague-Dawley rats (200-250 g) are used. 1 μg of CCL2 and/or 1 mM of INCB3344 is administered intrathecally between L5 and L6 vertebrae. Animals are tested once at 30, 60, 90, 120, and 240 min following drug administration. The percentage of maximal potential effect (MPE) is calculated for every time point.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Xue CB, et al. Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7473-8 [Content Brief]
[2]. Brodmerkel CM, et al. Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344. J Immunol. 2005 Oct 15;175(8):5370-8. [Content Brief]
[3]. Chan CT, et al. Reversal of vascular macrophage accumulation and hypertension by a CCR2 antagonist in deoxycorticosterone/salt-treated mice. Hypertension. 2012 Nov;60(5):1207-12. [Content Brief]
[4]. Dansereau MA, et al. Spinal CCL2 pronociceptive action is no longer effective in CCR2 receptor antagonist-treated rats. J Neurochem. 2008 Jul;106(2):757-69. [Content Brief]
[5]. Zhao W, et al. Enrichment of Ly6Chi monocytes by multiple GM-CSF injections with HBV vaccine contributes to viral clearance in a HBV mouse model. Hum Vaccin Immunother. 2017 Dec 2;13(12):2872-2882. [Content Brief]
[6]. Aye-Mon A, et al. CCR2 upregulation in DRG neurons plays a crucial role in gastric hyperalgesia associated with diabetic gastropathy. Mol Pain. 2018 Jan-Dec;14:1744806917751322. [Content Brief]
[7]. Cassini MF, et al. Mcp1 Promotes Macrophage-Dependent Cyst Expansion in Autosomal Dominant Polycystic Kidney Disease. J Am Soc Nephrol. 2018 Oct;29(10):2471-2481. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7313 mL | 8.6567 mL | 17.3133 mL | 43.2833 mL |
| 5 mM | 0.3463 mL | 1.7313 mL | 3.4627 mL | 8.6567 mL | |
| 10 mM | 0.1731 mL | 0.8657 mL | 1.7313 mL | 4.3283 mL | |
| 15 mM | 0.1154 mL | 0.5771 mL | 1.1542 mL | 2.8856 mL | |
| 20 mM | 0.0866 mL | 0.4328 mL | 0.8657 mL | 2.1642 mL | |
| 25 mM | 0.0693 mL | 0.3463 mL | 0.6925 mL | 1.7313 mL | |
| 30 mM | 0.0577 mL | 0.2886 mL | 0.5771 mL | 1.4428 mL | |
| 40 mM | 0.0433 mL | 0.2164 mL | 0.4328 mL | 1.0821 mL | |
| 50 mM | 0.0346 mL | 0.1731 mL | 0.3463 mL | 0.8657 mL | |
| 60 mM | 0.0289 mL | 0.1443 mL | 0.2886 mL | 0.7214 mL | |
| 80 mM | 0.0216 mL | 0.1082 mL | 0.2164 mL | 0.5410 mL | |
| 100 mM | 0.0173 mL | 0.0866 mL | 0.1731 mL | 0.4328 mL |
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