2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. Ilacirnon

Ilacirnon  (Synonyms: CCX140; CCX140-B)

Cat. No.: HY-101713 Purity: 99.87%
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CCX140 (CCX140-B) is a potent CCR2 antagonist.

For research use only. We do not sell to patients.

Ilacirnon Chemical Structure

Ilacirnon Chemical Structure

CAS No. : 1100318-47-5

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 196 In-stock
Solution
10 mM * 1 mL in DMSO USD 196 In-stock
Solid
2 mg USD 108 In-stock
5 mg USD 180 In-stock
10 mg USD 288 In-stock
50 mg USD 1020 In-stock
100 mg USD 1680 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Ilacirnon Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Ilacirnon

View All CCR Isoform Specific Products:

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

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

CCX140 (CCX140-B) is a potent CCR2 antagonist.

IC50 & Target[1]

hCCR2

2.3 nM (Kd, in monocytes)

CCR2

3 nM (IC50, in THP-1 cells)

CCR5

7 μM (IC50, in Activated T lymphocytes)

In Vitro

CCX140 (CCX140-B) potently inhibits CCL2-induced chemotaxis of purified human blood monocytes with IC50 values of 8 nM in buffer and 200 nM in the presence of 100% human serum. CCX140 also inhibits CCL2-induced Ca2+ mobilization in monocytes with an IC50 value of 3 nM. CCX140 inhibits the binding of 125I-CCL2 to monocytes with an IC50 value of 17 nM. CCX140 has a Kd value of 2.3 nM toward hCCR2. CCX140 also inhibits monocyte chemotaxis mediated by the other CCR2 ligands: CCL8/MCP-2, CCL7/MCP-3, and CCL13/MCP-4[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ilacirnon Related Antibodies
In Vivo

Treatment of hCCR2 KI mice with CCX140 (CCX140-B) causes a dose-dependent reduction in the number of peritoneal leukocytes after thioglycollate challenge: CCX140 strongly blocks leukocyte infiltration at 30 mg/kg, partially blocks leukocyte infiltration at 10 mg/kg, and fails to block leukocyte infiltration at 3 mg/kg. In DIO hCCR2 KI mice, treatment with 100 mg/kg CCX140 blocks the progressive increase in UAER and ACR. CCX140 maintains lower UAER and ACR values during the entire 8-wk dosing regimen[1]. In DIO mice, the CCR2 antagonist completely blocks the recruitment of inflammatory macrophages to visceral adipose tissue. The mice exhibit reduced hyperglycemia and insulinemia, improved insulin sensitivity, increased circulating adiponectin levels, decreased pancreatic islet size and increased islet number. CCX140 also reduces urine output, glucose excretion, hepatic glycogen and triglyceride content and glucose 6-phosphatase levels[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

495.86

Formula

C20H13ClF3N5O3S
CAS No.
Appearance

Solid

SMILES

FC(F)(F)C1=CC(S(=O)(NC2=CC(C)=CN=C2C(C3=NC=NC4=C3C=CN4)=O)=O)=CC=C1Cl
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: 

DMSO : ≥ 100 mg/mL (201.67 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 0.25 mg/mL (0.50 mM; Need ultrasonic and warming)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0167 mL 10.0835 mL 20.1670 mL
5 mM 0.4033 mL 2.0167 mL 4.0334 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.

* 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
=
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: ≥ 2.5 mg/mL (5.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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
Animal Administration
[1]

Mice: CCX140 is formulated as a solution in 1% hydroxypropyl methylcellulose. Male uninephrectomized hCCR2 KI mice are rendered diabetic with the high-fat diet and dosed with 100 mg/kg CCX140, but for 8 wk of dosing. Eight-week-old male hCCR2 KI Lepr db/db mice are similarly dosed with 100 mg/kg CCX140 for 6 wk[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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
DMSO 1 mM 2.0167 mL 10.0835 mL 20.1670 mL 50.4175 mL
5 mM 0.4033 mL 2.0167 mL 4.0334 mL 10.0835 mL
10 mM 0.2017 mL 1.0083 mL 2.0167 mL 5.0417 mL
15 mM 0.1344 mL 0.6722 mL 1.3445 mL 3.3612 mL
20 mM 0.1008 mL 0.5042 mL 1.0083 mL 2.5209 mL
25 mM 0.0807 mL 0.4033 mL 0.8067 mL 2.0167 mL
30 mM 0.0672 mL 0.3361 mL 0.6722 mL 1.6806 mL
40 mM 0.0504 mL 0.2521 mL 0.5042 mL 1.2604 mL
50 mM 0.0403 mL 0.2017 mL 0.4033 mL 1.0083 mL
60 mM 0.0336 mL 0.1681 mL 0.3361 mL 0.8403 mL
80 mM 0.0252 mL 0.1260 mL 0.2521 mL 0.6302 mL
100 mM 0.0202 mL 0.1008 mL 0.2017 mL 0.5042 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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Ilacirnon 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:

Ilacirnon1100318-47-5CCX140 CCX140-BCCX 140CCX-140CCRCC chemokine receptorInhibitorinhibitorinhibit

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