Home Tools
Log in
Cart

RS 504393

Catalog No. T5384   CAS 300816-15-3

RS 504393 is a highly selective CCR2 chemokine receptor antagonist (IC50s: 89 nM and < 100 μM for human recombinant CCR2 and CCR1).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
RS 504393 Chemical Structure
RS 504393, CAS 300816-15-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 43.00
5 mg In stock $ 98.00
10 mg In stock $ 168.00
25 mg In stock $ 369.00
50 mg In stock $ 553.00
100 mg In stock $ 798.00
1 mL * 10 mM (in DMSO) In stock $ 112.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 98.64%
Purity: 98.49%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description RS 504393 is a highly selective CCR2 chemokine receptor antagonist (IC50s: 89 nM and > 100 μM for human recombinant CCR2 and CCR1).
Targets&IC50 Human α1a receptor:72 nM (cell free), CCR2:89 nM (cell free)
In vitro RS-504393 inhibit MCP-1-stimulated calcium influx into CCR2-CHL cells. The IC50 values are 35 nM [1]. CCR2 antagonist, RS 504393 treatment, suppressed allergen induced β-hexosaminidase release significantly. This inhibitory effect was partially reversed by supplementation of recombinant MCP-1 protein (100 pg/mL) [2].
In vivo Whereas vehicle-treated mice developed clear signs of acute inflammation, RS 504393-treated mice failed to show clinical signs of immediate hypersensitivity. No effect was observed in naive animals. The degranulation of mast cells was significantly inhibited in RS 504393-treated mice but had no effect on naive mice [2]. Similar to the results obtained from CCR2-deficient mice, the treatment with RS-504393 significantly reduced renal pathology, especially the extensive interstitial fibrosis mediated by a decrease in type I collagen synthesis [3].
Kinase Assay Briefly, binding was measured using membranes prepared from two cell lines, THP-1 and CCR2-CHL cells. Each competition assay was composed of cell membranes, 50 pM 125I-MCP, MCP buffer, protease inhibitors, and test compound. Equilibrium was achieved by incubation at 28?°C for 90 min. Membrane-bound 125I-MCP was collected by filtration through GF/B filters presoaked in polyethyleneimine and bovine serum albumin, followed by four rapid washes with approximately 0.5 ml of ice-cold buffer containing 0.5 M NaCl and 10 mM HEPES, pH 7.4. MCP buffer consists of 50 mMHEPES, pH 7.2, 1 mM CaCl2, 5 mMMgCl2, and 0.1% bovine serum albumin. Protease inhibitors include 0.1 mM phenylmethylsulfonyl fluoride, 1 μM leupeptin, and 0.35 mg/ml pepstatin. THP-1 cells are a human monocyte cell line that express both CCR1 and CCR2. CCR2-CHL cells are Chinese hamster lung cells that have been stably transformed with an expression vector bearing the human CCR2b receptor [1].
Cell Research Briefly, cytosolic calcium influx was measured in CCR2-CHL cells loaded with the fluorescent dye Fura-2-AM. Quantitation of signal intensity used the integrated signal intensity for 82 s after the addition of chemokine and thus has units of M·s. Antagonism by various compounds of calcium influx was measured using an approximate ED50 dose of MCP-1 (3 nM) and an approximate ED25 dose for MCP-3 (5 nM). Chemotaxis was measured over 1 h using THP-1–5X cells in a 96-well Boyden chamber apparatus. Cell migration through the polycarbonate filter was quantified by fluorescent staining using propidium iodide in 0.1% Triton X-100. These assays typically gave stimulated to unstimulated migration of 6-fold, range 4–10-fold, using a maximally effective concentration of MCP-1. Chemotaxis antagonist measurements used 3 nM MCP-1 or RANTES; these concentrations are near the ED95 attractant concentration for MCP-1 and for RANTES as agonists. The data are expressed by normalization to the uninhibited migration caused by the agonist chemokine. The antagonist was present in both chambers of the Boyden apparatus [1].
Animal Research To evaluate the therapeutic effects of MCP-1/CCR2 signaling, either propagermanium (3 or 8 mg/kg orally once a day) or RS-504393 (2 mg/kg orally twice a day) was mandatorily injected into their mouths to wild-type mice from 3 days before ureteral ligation until the day of sacrifice. In addition, to determine the viability for the usage of CCR2 antagonists for the treatment of renal fibrosis, propagermanium (8 mg/kg) was given daily, beginning 4 days after ureter ligation. For pathological examination, both the obstructed and contralateral kidneys were harvested from UUO animals 4, 7, and 14 days after ureteral ligation (n = 5 at each time point). Untreated age-matched male wild-type mice and CCR2-deficient mice were used as normal control (n = 6 for each group). Since propagermanium treatment was started from 3 days before ureteral ligation, mice treated with propagermanium for 3 days at day 0 were used as a negative control (n = 5) [3].
Molecular Weight 417.5
Formula C25H27N3O3
CAS No. 300816-15-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (23.95 mM)

H2O: Insoluble

TargetMolReferences and Literature

1. Mirzadegan T, et al. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle. J Biol Chem. 2000 Aug 18;275(33):25562-71. 2. Tominaga T, et al. Blocking mast cell-mediated type I hypersensitivity in experimental allergic conjunctivitis by monocyte chemoattractant protein-1/CCR2. Invest Ophthalmol Vis Sci. 2009 Nov;50(11):5181-8. 3. Kitagawa K, et al. Blockade of CCR2 ameliorates progressive fibrosis in kidney. Am J Pathol. 2004 Jul;165(1):237-46.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Bioactive Compounds Library Max Immunology/Inflammation Compound Library Target-Focused Phenotypic Screening Library Chemokine Inhibitor Library GPCR Compound Library Immuno-Oncology Compound Library Bioactive Compound Library Nonsteroidal Anti-Inflammatory Compound Library Anti-COVID-19 Compound Library

Related Products

Related compounds with same targets
CCR8 antagonist 1 Aplaviroc Cenicriviroc AZD2098 Leronlimab TAK-779 5-Hydroxy-7,8-dimethoxyflavanone CCR2-RA-[R]

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

RS 504393 300816-15-3 Immunology/Inflammation Microbiology/Virology CCR CC chemokine receptor RS504393 Inhibitor inhibit RS-504393 inhibitor

 

TargetMol