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

C-021 is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM, respectively. C-021 effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor with an IC50 of 18 nM.

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C-021 Chemical Structure

C-021 Chemical Structure

CAS No. : 864289-85-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
1 mg USD 60 In-stock
5 mg USD 120 In-stock
10 mg USD 190 In-stock
25 mg USD 390 In-stock
50 mg USD 620 In-stock
100 mg USD 980 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of C-021:

C-021 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE C-021

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

C-021 is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM, respectively. C-021 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 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

467.65

Formula

C27H41N5O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

COC1=CC2=NC(N3CCC(N4CCCCC4)CC3)=NC(NC5CCCCCC5)=C2C=C1OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

Ethanol : 50 mg/mL (106.92 mM; ultrasonic and warming and heat to 60°C)

DMSO : 50 mg/mL (106.92 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1384 mL 10.6918 mL 21.3835 mL
5 mM 0.4277 mL 2.1384 mL 4.2767 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.71 mg/mL (1.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.71 mg/mL (1.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 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.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
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. 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
Ethanol / DMSO 1 mM 2.1384 mL 10.6918 mL 21.3835 mL 53.4588 mL
5 mM 0.4277 mL 2.1384 mL 4.2767 mL 10.6918 mL
10 mM 0.2138 mL 1.0692 mL 2.1384 mL 5.3459 mL
15 mM 0.1426 mL 0.7128 mL 1.4256 mL 3.5639 mL
20 mM 0.1069 mL 0.5346 mL 1.0692 mL 2.6729 mL
25 mM 0.0855 mL 0.4277 mL 0.8553 mL 2.1384 mL
30 mM 0.0713 mL 0.3564 mL 0.7128 mL 1.7820 mL
40 mM 0.0535 mL 0.2673 mL 0.5346 mL 1.3365 mL
50 mM 0.0428 mL 0.2138 mL 0.4277 mL 1.0692 mL
60 mM 0.0356 mL 0.1782 mL 0.3564 mL 0.8910 mL
80 mM 0.0267 mL 0.1336 mL 0.2673 mL 0.6682 mL
100 mM 0.0214 mL 0.1069 mL 0.2138 mL 0.5346 mL
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C-021 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-021864289-85-0C021C 021CCRCC chemokine receptorCCR4CCL22GTPγSchemotaxisInhibitorinhibitorinhibit

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