[CAS NO. 300816-15-3] RS504393
PRODUCTS SPECIFICATIONS [300816-15-3]
DESCRIPTION [300816-15-3]
Overview
| MDL | MFCD09038564 |
|---|---|
| Molecular Weight | 417.50 |
| Molecular Formula | C25H27N3O3 |
| SMILES | O=C1NC2=CC=C(C)C=C2C3(CCN(CCC4=C(C)OC(C5=CC=CC=C5)=N4)CC3)O1 |
8 Publications Citing Use of MCE
- [1]Nat Commun. 2022 Nov 26;13(1):7281.
- [2]Cell Death Dis. 2022 Aug 29;13(8):748.
- [3]Front Immunol. 2022 Jun 30;13:857311.
- [4]Front Immunol. 2022 Feb 4;13:835986.
- [5]Mol Immunol. 2019 May;109:140-148.
- [6]Cytokine. 2018 Oct;110:70-77.
- [7]Neurosci Lett. 2019 May 14;701:100-105.
- [8]In Vivo. Nov-Dec 2021;35(6):3053-3066.
Summary
RS 504393 is a selective CCR2 chemokine receptor antagonist ( IC 50 values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).
IC50 & Target
|
CCR2 89 nM (IC 50 ) |
Human α 1a receptor 72 nM (IC 50 ) |
Human α 1d receptor 460 nM (IC 50 ) |
5HT-1a receptor 1070 nM (IC 50 ) |
In Vitro
RS 504393 inhibits the MCP-1-induced chemotaxis with an IC 50 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
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
DMSO : 12.5 mg/mL ( 29.94 mM ; Need ultrasonic)
H 2 O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
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 |
References
- [1] Baamonde, Ana., et al. Involvement of glutamate NMDA and AMPA receptors, glial cells and IL-1β in the spinal hyperalgesia evoked by the chemokine CCL2 in mice. Neuroscience Letters (2011), 502(3), 178-181.
- [2] Yang, Dong., et al. Roles of CC chemokine receptors (CCRs) on lipopolysaccharide-induced acute lung injury. Respiratory Physiology & Neurobiology (2010), 170(3), 253-259.
- [3] Kitagawa, Kiyoki., et al. Blockade of CCR2 ameliorates progressive fibrosis in kidney. American Journal of Pathology (2004), 165(1), 237-246.
- [4] 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.
- [5] 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.