1. GPCR/G Protein Immunology/Inflammation
  2. CCR
  3. J-113863

J-113863 is a potent and selective CCR1 antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect.

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

J-113863 Chemical Structure

J-113863 Chemical Structure

CAS No. : 353791-85-2

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mg USD 210 In-stock
50 mg USD 680 In-stock
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Based on 3 publication(s) in Google Scholar

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Description

J-113863 is a potent and selective CCR1 antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect[1][2][3].

IC50 & Target[2][3]

CCR1

0.9 nM (IC50, Human CCR1)

CCR1

5.8 nM (IC50, Mouse CCR1)

CCR3

0.58 nM (IC50, Human CCR3)

CCR3

460 nM (IC50, Mouse CCR3)

In Vitro

Modified Vaccinia virus Ankara (MVA) but not MVA and vaccinia virus (VACV) infected MH-S cells increase the expression of the CXCR2 acting chemokine CXCL2. MH-S cells constitutively produce CCL2 and CCR1 acting chemokines CCL3, CCL5 and CCL9. Consequently, supernatants of mock treated and virus infected MH-S cells induce chemotaxis of murine promyelocyte MPRO cells and human monocytic THP-1 cells at the same level. However, supernatants of MVA infected MH-S cells significantly increase chemotaxis of the CCR2 deficient human monocytic cell line U-937. Chemotaxis of all above cell types is inhibited by J-113863[1].

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

In Vivo

J-113863 (3-10 mg/kg; intraperitoneal injection; once daily; for 11 days; DBA-1 male mice) treatment improves paw inflammation and joint damage, and dramatically decreases cell infiltration into joints in arthritic mice[2].

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

Animal Model: DBA-1 male mice (10-12 weeks) induced with Collagen[2]
Dosage: 3 mg/kg, 10 mg/kg
Administration: Intraperitoneal injection; once daily; for 11 days
Result: Improved paw inflammation and joint damage, and dramatically decreased cell infiltration into joints.
Molecular Weight

655.44

Formula

C30H37Cl2IN2O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(C3C4=C(OC5=C3C=C(Cl)C=C5)C=CC(Cl)=C4)=O)CC1.[I-]

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 : 50 mg/mL (76.28 mM; Need ultrasonic; 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 1.5257 mL 7.6285 mL 15.2569 mL
5 mM 0.3051 mL 1.5257 mL 3.0514 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.

  • 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 (3.81 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (3.81 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 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

Purity: ≥99.0%

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
DMSO 1 mM 1.5257 mL 7.6285 mL 15.2569 mL 38.1423 mL
5 mM 0.3051 mL 1.5257 mL 3.0514 mL 7.6285 mL
10 mM 0.1526 mL 0.7628 mL 1.5257 mL 3.8142 mL
15 mM 0.1017 mL 0.5086 mL 1.0171 mL 2.5428 mL
20 mM 0.0763 mL 0.3814 mL 0.7628 mL 1.9071 mL
25 mM 0.0610 mL 0.3051 mL 0.6103 mL 1.5257 mL
30 mM 0.0509 mL 0.2543 mL 0.5086 mL 1.2714 mL
40 mM 0.0381 mL 0.1907 mL 0.3814 mL 0.9536 mL
50 mM 0.0305 mL 0.1526 mL 0.3051 mL 0.7628 mL
60 mM 0.0254 mL 0.1271 mL 0.2543 mL 0.6357 mL
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J-113863 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.

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J-113863
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