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C-021
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Catalog No. T21870Cas No. 864289-85-0
Alias 4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-
C 021 dihydrochloride is a potent CCR4 antagonist. C-021 (4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-) dihydrochloride potently inhibits functional chemotaxis in humans and mice with IC50s of 140 nM and 39 nM, respectively. It effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor (IC50: 18 nM).
C-021
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Purity: 99.90%
Catalog No. T21870Alias 4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-Cas No. 864289-85-0
C 021 dihydrochloride is a potent CCR4 antagonist. C-021 (4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-) dihydrochloride potently inhibits functional chemotaxis in humans and mice with IC50s of 140 nM and 39 nM, respectively. It effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor (IC50: 18 nM).
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $47 | In Stock | In Stock | |
| 2 mg | $65 | In Stock | In Stock | |
| 5 mg | $97 | In Stock | In Stock | |
| 10 mg | $155 | In Stock | In Stock | |
| 25 mg | $318 | In Stock | In Stock | |
| 50 mg | $493 | In Stock | In Stock | |
| 100 mg | $690 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $97 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:99.90%
Appearance:Solid
Color:White
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Product Introduction
C-021 AI Summary
C-021 has been characterized for various pharmacological activities and metabolic properties. It exhibits potent antagonist activity at both human and mouse CCR4 receptors, demonstrating inhibition of CCL22-induced chemotaxis and [35S]GTPgammaS binding in mouse B300-19 cells, with IC50 values of 18.0 nM and 39.0 nM, respectively. For human CCR4 receptors, IC50 values are 140.0 nM for CCL22-induced chemotaxis. Metabolic studies indicate a high intrinsic clearance in human liver microsomes, with a CL value of 289.62 mL.min^-1.kg^-1, suggesting a rapid metabolism and potentially short half-life in vivo.
In addition to its CCR4 receptor antagonist activity, C-021 shows anti-inflammatory properties by inhibiting oxazolone-induced contact hypersensitivity in a BALB/c mouse model, reducing ear swelling by 2.0% at an oral dose of 30 mg/kg twice daily. The compound also exhibits antiviral activity against SARS-CoV-2, inhibiting virus-induced cytotoxicity in Caco-2 cells with a 6.45% inhibition rate at 10 µM concentration over 48 hours, and showing minimal inhibition of cytotoxicity in VERO-6 cells under similar conditions. Moreover, it inhibits the SARS-CoV-2 3CL-Pro protease by -16.53% at a concentration of 20 µM.
Furthermore, C-021 displays inhibitory activity against human HDAC6 enzyme in enzymatic assays, though with relatively low inhibition percentages of 0.07% and 0.13% using different peptide substrates. This diverse range of activities highlights its potential utility in therapeutic applications across various fields, including immunology, virology, and inflammation..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | C 021 dihydrochloride is a potent CCR4 antagonist. C-021 (4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-) dihydrochloride potently inhibits functional chemotaxis in humans and mice with IC50s of 140 nM and 39 nM, respectively. It effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor (IC50: 18 nM). |
| Targets&IC50 | CCR4:140 nM (human), CCR4:39 nM(mice) |
| Synonyms | 4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy- |
| Molecular Weight | 467.65 |
| Formula | C27H41N5O2 |
| Cas No. | 864289-85-0 |
| Smiles | N(C=1C2=C(N=C(N1)N3CCC(CC3)N4CCCCC4)C=C(OC)C(OC)=C2)C5CCCCCC5 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 9 mg/mL (19.25 mM), Sonication is recommended.  | ||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 0.5 mg/mL (1.07 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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