RS504393 free base · Synonyms: RS-504393 · RS 504393

RS 504393 is a selective CCR2 chemokine receptor antagonist.

For research use only. Not for human or veterinary use.

Target CCR

Research area Inflammation/Immunology Endocrinology

Purity >98% Stock Inquire

Data Sheet SDS COA

RS504393 structure

CAS No.: 300816-15-3

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 498.00	BP-02253-250mg	In stock	Get quote
500 mg	USD 750.00	BP-02253-500mg	In stock	Get quote
1 g	USD 1,350.00	BP-02253-1g	In stock	Get quote
2 g	USD 2,200.00	BP-02253-2g	In stock	Get quote
5 g	Inquire	BP-02253-5g	In stock	Inquire

Need another size or custom synthesis? Request a quote.

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).

Biological activity

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. 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.

Identifiers

SMILES: CC1=CC2=C(C=C1)NC(=O)OC23CCN(CC3)CCC4=C(OC(=N4)C5=CC=CC=C5)C
InChIKey: ODNICNWASXKNNQ-UHFFFAOYSA-N

Specifications

MW (average): 417.5002
Formula: C₂₅H₂₇N₃O₃
CAS No.: 300816-15-3
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 year

Solubility

Soluble in DMSO

In vitro: DMSO : 10 mg/mL

Documents

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.

Same research area

Search Inflammation/Immunology