RS 102895 hydrochloride
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.
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 426.86. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.34 mL||11.71 mL||23.43 mL|
|5 mM||0.47 mL||2.34 mL||4.69 mL|
|10 mM||0.23 mL||1.17 mL||2.34 mL|
|50 mM||0.05 mL||0.23 mL||0.47 mL|
References are publications that support the products' biological activity.
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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2 Citations for RS 102895 hydrochloride
Citations are publications that use Tocris products. Selected citations for RS 102895 hydrochloride include:
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
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
Do you know of a great paper that uses RS 102895 hydrochloride from Tocris? If so please let us know.
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