INCB 3284 dimesylate
Based on 2 publication(s) in Google Scholar
INCB 3284 dimesylate is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 dimesylate can be used in the research of acute liver failure.
For research use only. We do not sell to patients.
- CAS No.: 887401-93-6
- Formula: C28H39F3N4O10S2
- Molecular Weight:712.76
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) INCB 3284 dimesylate
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Biological Activity
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MCP-1-hCCR2 3.7 nM (IC50) |
INCB 3284 dimesylate is a pentent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 also causes an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 μM in inhibition of the hERG potassium current. However, INCB 3284 has no effec on CCR1, CCR3, CCR5, CXCR3, and CXCR5, or additional GPCRs at a concentration of 1 μM. Moreover, INCB 3284 potently inhibits CCR2-mediated signaling events such as intracellular calcium mobilization and ERK phosphorylation with IC50 values of 6 and 2.6 nM, respectively[1].
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. 887401-93-6
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Appearance Oil
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Molecular Weight 712.76
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Formula C28H39F3N4O10S2
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Color Colorless to light yellow
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SMILES
O=C(NCC(N[C@H]1CN([C@H]2CC[C@](C3=CC=C(OC)N=C3)(O)CC2)CC1)=O)C4=CC=CC(C(F)(F)F)=C4.CS(=O)(O)=O.CS(=O)(O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Acta Pharm Sin B
Choroid plexus CCL2‒CCR2 signaling orchestrates macrophage recruitment and cerebrospinal fluid hypersecretion in hydrocephalus. [Abstract]2024 Oct;14(10):4544-4559. PMID: 39525574 -
Cell Commun Signal
Targeting CCL2-CCR2 signaling pathway alleviates macrophage dysfunction in COPD via PI3K-AKT axis. [Abstract]2024 Jul 17;22(1):364. PMID: 39014433
Solvent & Solubility
DMSO : ≥ 83.3 mg/mL (116.87 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Protocol
Mice[2]
Male C57Bl/6 mice (20 to 25 g) are given free access to water and rodent chow and are housed in constant temperature, humidity, and 12 h light-dark cycling. Acute liver failure is induced via a single intraperitoneal (ip) injection of 100 mg/kg of azoxymethane (AOM). In parallel, systemic inhibition of CCR2 and CCR4 activity is accomplished via pretreatment with INCB 3284 (1 mg/kg/day ip) or C021 (1 mg/kg/day ip) for 3 days prior to injection of AOM. Following injection, mice are placed on heating pads adjusted to 37°C and monitored frequently for signs of neurological decline. To reduce the impacts of hypoglycemia and dehydration, cage floors are supplied with hydrogel and rodent chow and after 12 h, and every subsequent 4 h, mice are injected subcutaneously with 5% dextrose in 250 μL of saline. If mice undergo a 20% or greater weight loss they are removed from the study[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Xue CB, et al. Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist. ACS Med Chem Lett. 2011 Mar 31;2(6):450-4. [Content Brief]
[2]. McMillin M, et al. Neuronal CCL2 is upregulated during hepatic encephalopathy and contributes to microglia activation and neurological decline. J Neuroinflammation. 2014 Jul 10;11:121. [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 (sealed storage, away from moisture). 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 | 1.4030 mL | 7.0150 mL | 14.0300 mL | 35.0749 mL |
| 5 mM | 0.2806 mL | 1.4030 mL | 2.8060 mL | 7.0150 mL | |
| 10 mM | 0.1403 mL | 0.7015 mL | 1.4030 mL | 3.5075 mL | |
| 15 mM | 0.0935 mL | 0.4677 mL | 0.9353 mL | 2.3383 mL | |
| 20 mM | 0.0701 mL | 0.3507 mL | 0.7015 mL | 1.7537 mL | |
| 25 mM | 0.0561 mL | 0.2806 mL | 0.5612 mL | 1.4030 mL | |
| 30 mM | 0.0468 mL | 0.2338 mL | 0.4677 mL | 1.1692 mL | |
| 40 mM | 0.0351 mL | 0.1754 mL | 0.3507 mL | 0.8769 mL | |
| 50 mM | 0.0281 mL | 0.1403 mL | 0.2806 mL | 0.7015 mL | |
| 60 mM | 0.0234 mL | 0.1169 mL | 0.2338 mL | 0.5846 mL | |
| 80 mM | 0.0175 mL | 0.0877 mL | 0.1754 mL | 0.4384 mL | |
| 100 mM | 0.0140 mL | 0.0701 mL | 0.1403 mL | 0.3507 mL |
INCB 3284 dimesylate Related Classifications
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