C-021 Dihydrochloride | CCR4 Antagonist - MedChemExpress
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- C-021 dihydrochloride
Solubility
In Vivo Dissolution Calculator
Help & FAQs
C-021 dihydrochloride is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 dihydrochloride potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM, respectively. C-021 dihydrochloride effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor with an IC50 of 18 nM.
For research use only. We do not sell to patients.
C-021 dihydrochloride Chemical Structure
CAS No. : 1784252-84-1
| Size | Price | Stock | Quantity |
|---|---|---|---|
| Solid + Solvent (Highly Recommended) | |||
| 10 mM * 1 mL in DMSO ready for reconstitution | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 | |
| Solution | |||
| 10 mM * 1 mL in DMSO | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 | |
| Solid | |||
| 1 mg | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 | |
| 5 mg | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 | |
| 10 mg | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 | |
| 50 mg | Get quote | ||
| 100 mg | Get quote | ||
* Please select Quantity before adding items.
This product is a controlled substance and not for sale in your territory.
Customer Review
Based on 2 publication(s) in Google Scholar
Other Forms of C-021 dihydrochloride:
- C-021 In-stock
- C-021 dihydrochloride (Standard) Get quote
C-021 dihydrochloride Related Antibodies
2 Publications Citing Use of MCE C-021 dihydrochloride
- •J Immunother Cancer. 2024 Dec 4;12(12):e009629. [Abstract]
- •Biochem Pharmacol. 2023 Apr:210:115475. [Abstract]
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View All CCR Isoform Specific Products:
View All Isoforms CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9Biological Activity
Purity & Documentation
References
Customer Review
| Description | C-021 dihydrochloride is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 dihydrochloride potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM, respectively. C-021 dihydrochloride effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor with an IC50 of 18 nM[1]. | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| IC50 & Target[1] |
| ||||||||||||
| In Vitro | The in vitro oxidative metabolic stability of C-021 (Compound 1b) is evaluated by measuring the rate of drug consumption in human liver microsomes (HML), thus providing intrinsic clearance values (CLint). C-021 exhibits CLint value of 17,377 mL/h/kg[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. C-021 dihydrochloride Related Antibodies | ||||||||||||
| In Vivo | The potency of C-021 (Compound 1b) is evident after subcutaneous administration in the murine oxazolone-induced contact hypersensitivity test, a known model of acute skin inflammation. When C-021 is administered orally, however, very little inhibition is observed[1]. C-021 (1 mg/kg; i.p.; daily; for 3 days) significantly less microgliosis in acute liver failuremice[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| ||||||||||||
| Molecular Weight | 540.57 | ||||||||||||
| Formula | C27H43Cl2N5O2 | ||||||||||||
| CAS No. | 1784252-84-1 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Color | White to off-white | ||||||||||||
| SMILES | COC1=CC2=NC(N3CCC(N4CCCCC4)CC3)=NC(NC5CCCCCC5)=C2C=C1OC.[H]Cl.[H]Cl | ||||||||||||
| Shipping | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||
| Solvent & Solubility | In Vitro: DMSO : 83.33 mg/mL (154.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O : 27.0285 mg/mL (50.00 mM; Need ultrasonic and warming) Preparing Stock Solutions
* 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. * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Mass kg g mg μg ng pg = Concentration M mM μM nM pM × Volume L mL μL × Molecular Weight *Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 Concentration (start) M mM μM nM pMC1 × Volume (start) L mL μLV1 = Concentration (final) M mM μM nM pMC2 × Volume (final) L mL μLV2 In Vivo Dissolution Calculator Please enter the basic information of animal experiments:Dosage mg/kgAnimal weight (per animal) gDosing volume (per animal) μLNumber of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments. Calculation results: Working solution concentration: mg/mL This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details. The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE). Tel: 609-228-6898 E-mail: [email protected] Technical Support: [email protected] | ||||||||||||
| Purity & Documentation | Purity: 99.92% Select Batch: HY-103364A-57458 HY-103364A-908705 HY-103364A-980069 HY-103364A-532067 HY-103364A-1038049 Data Sheet (277 KB) SDS (393 KB)COA (253 KB) LCMS (94 KB) Handling Instructions (2659 KB) | ||||||||||||
| References |
|
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[1]. Yokoyama K, et al. Potent and orally bioavailable CCR4 antagonists: Synthesis and structure-activity relationship study of 2-aminoquinazolines. Bioorg Med Chem. 2009 Jan 1;17(1):64-73.
[2]. Matthew McMillin, et al. Neuronal CCL2 is upregulated during hepatic encephalopathy and contributes to microglia activation and neurological decline. J Neuroinflammation. 2014 Jul 10;11:121.
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 |
|---|
| H2O / DMSO | 1 mM | 1.8499 mL | 9.2495 mL | 18.4990 mL | 46.2475 mL |
| 5 mM | 0.3700 mL | 1.8499 mL | 3.6998 mL | 9.2495 mL | |
| 10 mM | 0.1850 mL | 0.9249 mL | 1.8499 mL | 4.6247 mL | |
| 15 mM | 0.1233 mL | 0.6166 mL | 1.2333 mL | 3.0832 mL | |
| 20 mM | 0.0925 mL | 0.4625 mL | 0.9249 mL | 2.3124 mL | |
| 25 mM | 0.0740 mL | 0.3700 mL | 0.7400 mL | 1.8499 mL | |
| 30 mM | 0.0617 mL | 0.3083 mL | 0.6166 mL | 1.5416 mL | |
| 40 mM | 0.0462 mL | 0.2312 mL | 0.4625 mL | 1.1562 mL | |
| DMSO | 60 mM | 0.0308 mL | 0.1542 mL | 0.3083 mL | 0.7708 mL |
| 80 mM | 0.0231 mL | 0.1156 mL | 0.2312 mL | 0.5781 mL | |
| 100 mM | 0.0185 mL | 0.0925 mL | 0.1850 mL | 0.4625 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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C-021 dihydrochloride Related Classifications
- Disease Areas
- Inflammation or Immune System Disease Digestive System Disease Respiratory Disease Musculoskeletal Disease Cancer
- Pulmonary Disease Autoimmune Disease Arthritis Digestive System Inflammation
- Lung Fibrosis Rheumatoid Arthritis
- Inflammation/Immunology
- GPCR/G Protein Immunology/Inflammation
- CCR
- Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
C-0211784252-84-1C021C 021CCRCC chemokine receptorCCR4CCL22GTPγSchemotaxisInhibitorinhibitorinhibit
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