RS 102895 hydrochloride

Cat. No. 2089

RS 102895 hydrochloride C21H21F3N2O2.HCl [1173022-16-6]

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Chemical Name: 1'-[2-[4-(Trifluoromethyl)phenyl]ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one hydrochloride

Biological Activity

CCR2-selective chemokine receptor antagonist (IC50 values are 0.36 and 17.8 μM for inhibition of human recombinant CCR2b and CCR1 receptors respectively). Blocks MCP-1-stimulated calcium influx and chemotaxis with IC50 values of 32 nM and 1.7 μM respectively. Also inhibits α1A, α1D and 5-HT1A receptors.

Technical Data

M.Wt:
426.86
Formula:
C21H21F3N2O2.HCl
Solubility:
Soluble to 75 mM in DMSO
Purity:
>99 %
Storage:
Desiccate at RT
CAS No:
1173022-16-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

Mirzadegan et al (2000) Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists. J.Biol.Chem. 275 25562. PMID: 10770925.

Clark et al (1983) Synthesis and antihypertensive activity of 4'-substituted spiro[4H-3,1-benzoxazine-4,4'piperidin]-2(1H)-ones. J.Med.Chem. 26 657. PMID: 6842505.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for RS 102895 hydrochloride include:

Maxwell et al (2014) Tumor-derived CXCL8 signaling augments stroma-derived CCL2-promoted proliferation and CXCL12-mediated invasion of PTEN-deficient prostate cancer cells. Oncotarget 5 4895. PMID: 24970800.

Sennlaub et al (2013) CCR2(+) monocytes infiltrate atrophic lesions in age-related macular disease and mediate photoreceptor degeneration in experimental subretinal inflammation in Cx3cr1 deficient mice. EMBO Mol Med 5 1775. PMID: 24142887.

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Keywords: RS 102895 hydrochloride, supplier, CCR2b, chemokine, receptor, antagonists, Chemokine, Receptors, RS102895, hydrochloride, Tocris Bioscience, Chemokine CC Receptor Antagonist products

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