C-021 Dihydrochloride | CCR4 Antagonist - MedChemExpress

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                                1. GPCR/G Protein Immunology/Inflammation
                                2. CCR
                                3. C-021 dihydrochloride
                                C-021 dihydrochloride Cat. No.: HY-103364A Purity: 99.92% Data Sheet COA SDS Handling Instructions FAQs Technical Support

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                                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

                                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
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                                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

                                Top Publications Citing Use of Products

                                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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                                Related Small Molecules:

                                Related Proteins:

                                View All CCR Isoform Specific Products:

                                View All Isoforms CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9
                                • Biological 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]

                                CCR4

                                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.

                                Animal Model: Male C57Bl/6 mice (20-25 g) with acute liver failure[2]
                                Dosage: 1 mg/kg
                                Administration: i.p.; daily; for 3 days
                                Result: Significantly less microgliosis, and significantly reduced the pERK1/2 to tERK1/2 ratio.
                                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
                                Concentration Solvent Mass 1 mg 5 mg 10 mg
                                1 mM 1.8499 mL 9.2495 mL 18.4990 mL
                                5 mM 0.3700 mL 1.8499 mL 3.6998 mL
                                10 mM 0.1850 mL 0.9249 mL 1.8499 mL
                                View the 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.

                                * 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.

                                • Molarity Calculator

                                • Dilution Calculator

                                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 pM

                                C1

                                × Volume (start) L mL μL

                                V1

                                = Concentration (final) M mM μM nM pM

                                C2

                                × Volume (final) L mL μL

                                V2

                                In Vivo Dissolution Calculator Please enter the basic information of animal experiments:

                                Dosage

                                mg/kg

                                Animal weight (per animal)

                                g

                                Dosing volume (per animal)

                                μL

                                Number 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
                                • [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. [Content Brief]

                                  [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. [Content Brief]

                                • [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
                                Help & FAQs
                                • 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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