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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 887401-93-6
- Fòrmula: C28H39F3N4O10S2
- Peso molecular:712.76
-
Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
HY-15418
RS 504393CCR2 Antagonist -
HY-50674
INCB3344CCR2 Antagonis -
HY-13245
PF-4136309CCR2 Antagonist -
HY-50669
MK-0812CCR Antagonist -
HY-12080
BX471CCR1 Antagonist -
HY-13004
MaravirocCCR5 Antagonist -
HY-12080A
BX471 hydrochlorideCCR Antagonist -
HY-18611
Abaucin hydrochlorideCCR2antagonist -
HY-18611A
AbaucinCCR Antagonist -
HY-103361
SB297006CCR3 Antagonist -
HY-109593
BMS-813160CCR2/CCR5 Antagonist -
HY-108323
CCR2 antagonist 4CCR2b Antagonist
Publications Citing Use of MedChemExpress (MCE) INCB 3284 dimesylate
More
Actividad biológica
Descripciòn
IC50 & Target
[1]|
MCP-1-hCCR2 3.7 nM (IC50) |
In Vitro
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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
No. CAS 887401-93-6
-
Appearance Oil
-
Peso molecular 712.76
-
Fòrmula C28H39F3N4O10S2
-
Color Colorless to light yellow
-
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
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
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
Solvente y solubilidad
In Vitro:
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)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Pureza y Documentación
-
Ficha de datos (275 KB)
-
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)
-
Instrucciones de manejo (2659 KB)
Referencias
[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
HY-15450 Related Classifications
Powered by Bioz