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RS 102895 hydrochloride

Cat. No. 2089

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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 α_1A, α_1D and 5-HT_1A 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:

300815-41-2

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

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.

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.

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