CCG258747
Based on 1 publication(s) in Google Scholar
CCG258747 is a selective GRK2 inhibitor (IC50 = 18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, > 5500, and > 550-fold, respectively). CCG258747 also blocks the internalization of the µ-opioid receptor (MOR). CCG258747 attenuates IgE mediated anaphylaxis by inhibiting GRK2 and FcεRI signaling pathway but activates mast cells via MRGPRX2 and MRGPRB2. CCG258747 can be used to study diseases related to overexpression of GRK2 (such as heart failure, opioid tolerance).
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- Pureza: 98.96%
- No. CAS: 2615910-00-2
- Fòrmula: C28H27FN4O4
- Peso molecular:502.54
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Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) CCG258747
MoreVer todos los productos específicos de isoformas Opioid Receptor
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Actividad biológica
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GRK2 18 nM (IC50) |
μ Opioid Receptor/MOR |
CCG258747 (20 μM, 10-20 min) effectively penetrates the cell membrane (HEK293 and U2OS cells) and inhibit the GRK2 activity within the cells, thereby blocking the MOR internalization process mediated by GRK2, and this process does not occur by inhibiting the phosphorylation of Ser375[1].
CCG258747 (1-30 μM, 30 min) inhibits FcϵRI-mediated calcium mobilization and degranulation in RBL-2H3 cells[2].
CCG258747 (10-30 μM) inhibits IgE-mediated degranulation in primary mouse lung MCs (LMCs) and WT mice peritoneal MCs (PMCs), but the effect is very weak in the PMCs of Mrgprb2⁻/⁻ mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 and U2OS cells
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Concentration:20 μM
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Incubation Time:20 min
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Result:Did not significantly reduce the phosphorylation level of pSer375.
| Species | Dose | Route | AUC0-t | Plasma Concentration |
|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 5.97 μM·h | 0.43 μM |
CCG258747 (20 µg (0.1 mg/kg), i.d. in left hind paw, single dose) mediates local mast cell activation through MRGPRB2, but does not cause dangerous systemic allergic reactions[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Passive skin allergic reaction model established in WT and Mrgprb2⁻/⁻ mice[2]
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Dosage:5 mg/kg
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Administration:Intravenous injection (i.v.), single dose
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Result:Significantly reduced vascular permeability compared to untreated mice.
Did not cause a severe systemic allergic reaction.
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Animal Model:Verification model for the activating effect of MRGPRB2 established in WT and Mrgprb2⁻/⁻ mice[2]
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Dosage:20 µg (0.1 mg/kg)
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Administration:Intracutaneous injection (i.d.) in left hind paw, single dose
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Result:Caused significant dye extravasation (increased vascular permeability) in WT mice, but the effect was significantly reduced in Mrgprb2⁻/⁻ mice.
Chemical Information
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No. CAS 2615910-00-2
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Appearance Solid
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Peso molecular 502.54
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Fòrmula C28H27FN4O4
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Color Off-white to light yellow
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SMILES
O=C(NCC1=NNC2=CC=CC=C12)C(C=C3[C@@](CCNC4)([H])[C@@H]4COC5=CC=C(OCO6)C6=C5)=C(C=C3)F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Commun Biol
Cell-based and isoform-selective G protein-coupled receptor kinase assays for comprehensive inhibitor evaluation. [Abstract]2026 Jan 16;9(1):287. PMID: 41545717
Solvente y solubilidad
DMSO : 100 mg/mL (198.99 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 (sealed storage, away from moisture and light). 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 and light). 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: ≥ 2.5 mg/mL (4.97 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (4.97 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.
Pureza y Documentación
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Ficha de datos (285 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Renee A Bouley, et al. A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of the μ-Opioid Receptor. Mol Pharmacol. 2020 Jun;97(6):392-401. [Content Brief]
[2]. Thapaliya M, et al. GRK2 inhibitors, paroxetine and CCG258747, attenuate IgE-mediated anaphylaxis but activate mast cells via MRGPRX2 and MRGPRB2. Front Immunol. 2022 Oct 6;13:1032497. [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 and light). 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 | 1.9899 mL | 9.9495 mL | 19.8989 mL | 49.7473 mL |
| 5 mM | 0.3980 mL | 1.9899 mL | 3.9798 mL | 9.9495 mL | |
| 10 mM | 0.1990 mL | 0.9949 mL | 1.9899 mL | 4.9747 mL | |
| 15 mM | 0.1327 mL | 0.6633 mL | 1.3266 mL | 3.3165 mL | |
| 20 mM | 0.0995 mL | 0.4975 mL | 0.9949 mL | 2.4874 mL | |
| 25 mM | 0.0796 mL | 0.3980 mL | 0.7960 mL | 1.9899 mL | |
| 30 mM | 0.0663 mL | 0.3316 mL | 0.6633 mL | 1.6582 mL | |
| 40 mM | 0.0497 mL | 0.2487 mL | 0.4975 mL | 1.2437 mL | |
| 50 mM | 0.0398 mL | 0.1990 mL | 0.3980 mL | 0.9949 mL | |
| 60 mM | 0.0332 mL | 0.1658 mL | 0.3316 mL | 0.8291 mL | |
| 80 mM | 0.0249 mL | 0.1244 mL | 0.2487 mL | 0.6218 mL | |
| 100 mM | 0.0199 mL | 0.0995 mL | 0.1990 mL | 0.4975 mL |
CCG258747 Related Classifications
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