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  3. RS 504393

RS 504393 

Cat. No.: HY-15418 Purity: 99.18%
Handling Instructions

RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).

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

RS 504393 Chemical Structure

RS 504393 Chemical Structure

CAS No. : 300816-15-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 125 In-stock
Estimated Time of Arrival: December 31
5 mg USD 114 In-stock
Estimated Time of Arrival: December 31
10 mg USD 186 In-stock
Estimated Time of Arrival: December 31
25 mg USD 408 In-stock
Estimated Time of Arrival: December 31
50 mg USD 732 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

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Description

RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).

IC50 & Target[5]

CCR2

89 nM (IC50)

Human α1a receptor

72 nM (IC50)

Human α1d receptor

460 nM (IC50)

5HT-1a receptor

1070 nM (IC50)

In Vitro

RS 504393 inhibits the MCP-1-induced chemotaxis with an IC50 of 330 nM. RS 504393 treatment suppresses allergen induced β-hexosaminidase release significantly. Without allergen priming, MCP-1 induces mast cell degranulation, which is completely suppressed by RS 504393[4].

In Vivo

RS504393 (0.3-3 μg) with CCL2 progressively blocks thermal hyperalgesia dose-dependently in mice[1]. RS 504393 (5 mg/kg, i.v.) supresses the elevated numbers of leukocytes and increased total protein content in BALF induced by The LPS. RS504393 significantly down regulates the LPS-induced elevation of IL-1β, PAI-1 mRNA and protein expressions. RS504393 significantly suppresses induced lung edema, protein-rich fluid, polymorphonuclear accumulation and bronchial wall thickening induced by LPS[2]. RS-504393 significantly reduces renal pathology, especially the extensive interstitial fibrosis mediated by decrease in type I collagen synthesis in a UUO model[3].

Molecular Weight

417.50

Formula

C₂₅H₂₇N₃O₃

CAS No.

300816-15-3

SMILES

O=C1NC2=CC=C(C)C=C2C3(CCN(CCC4=C(C)OC(C5=CC=CC=C5)=N4)CC3)O1

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 : 12.5 mg/mL (29.94 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3952 mL 11.9760 mL 23.9521 mL
5 mM 0.4790 mL 2.3952 mL 4.7904 mL
10 mM 0.2395 mL 1.1976 mL 2.3952 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 1.25 mg/mL (2.99 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.25 mg/mL (2.99 mM); Clear solution

  • 3.

    Add each solvent one by one:  50% DMSO    15% EtOH    35% PEG300

    Solubility: 31.25 mg/mL (74.85 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[4]

Isolated mast cells are sensitized by incubation with anti-DNP IgE in RPMI1640 containing 10 ng/mL of murine recombinant IL-3, 10 ng/mL of recombinant SCF, and 5% murine serum. The cells are then washed with HBSS containing 10 ng/mL of murine recombinant IL-3, 10 ng/mL of recombinant SCF, 0.04% BSA, and 10 mM HEPES. Resuspended cells at a concentration of 2 to 8×104 cells/100 μL are transferred into triplicate wells of a 96 well U-bottom plate and allowed to equilibrate at 37°C for 10 minutes before the addition of DNP-albumin or compound 48/80. After 45 minutes, the plate is centrifuged at 290 g for 5 minutes at 4°C. The β-hexosaminidase activity of the culture supernatant is determined using a Published protocol. Fifty-μL aliquots of the supernatant are placed in wells of another 96-well plate together with 100 μL of 2.5 mM p-nitrophenyl-N-acetyl β-d glucosaminide solubilized in 0.04mol/Lcitrate buffer adjusted to pH 4.5 with disodium phosphate. After incubation at 37°C for 90 minutes, the reactions are terminated by addition of 50 μL of 0.4mol/Lglycin adjusted to pH 10.7 with sodium hydroxide. The colored product is measured at 405 nm with a reference filter of 570 nm. The relative release of β-hexosaminidase is defined as the activity in the supernatant of the tested cells divided by the activity in the positive control cell supernatant, multiplied by 100. Compound 48/80 stimulus is used for assay control.

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

Animal Administration
[2]

Male C57BL/6J mice (n=30) and male homozygote CCR1, CCR2 and CCR3 knockout mice (n=12, in each phenotype), 6-8 weeks old and weighing 20±2 g. Intranasal administration of PBS or LPS (5 mg/kg) is performed in a volume of 1 mL/kg body weight. C57BL/6J mice are treated with vehicle or RS504393 (5 mg/kg) intraperitoneally 30 min before LPS challenge. Four hours after LPS challenge, mice are terminated by an intraperitoneal injection of an overdose of pentobarbitone. The mice are kept on a 12-h light/dark cycle with access to mice chow and water ad libitum.

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

References

Purity: 99.18%

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Keywords:

RS 504393RS504393RS-504393CCRCC chemokine receptorInhibitorinhibitorinhibit

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RS 504393
Cat. No.:
HY-15418
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