2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. C-021 dihydrochloride

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.

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C-021 dihydrochloride Chemical Structure

C-021 dihydrochloride Chemical Structure

CAS No. : 1784252-84-1

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5 mg USD 350 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of C-021 dihydrochloride:

C-021 dihydrochloride Related Antibodies

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1 Publications Citing Use of MCE C-021 dihydrochloride

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  • Purity & Documentation

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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.
Unlabeled CAS

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 : 54.05 mg/mL (99.99 mM; Need ultrasonic and warming; 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
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
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

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).
Purity & Documentation
References

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

* 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

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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