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Submit ReviewRS 102895 hydrochloride
Description: CCR2b chemokine receptor antagonist
Chemical Name: 1'-[2-[4-(Trifluoromethyl)phenyl]ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for RS 102895 hydrochloride
RS 102895 hydrochloride is a 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.
Compound Libraries for RS 102895 hydrochloride
RS 102895 hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for RS 102895 hydrochloride
| M. Wt | 426.86 |
| Formula | C21H21F3N2O2.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 1173022-16-6 |
| PubChem ID | 16759153 |
| InChI Key | KRRISOFSWVKYBF-UHFFFAOYSA-N |
| Smiles | Cl.FC(F)(F)C1=CC=C(CCN2CCC3(CC2)OC(=O)NC2=CC=CC=C32)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for RS 102895 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.01 | 75 |
Preparing Stock Solutions for RS 102895 hydrochloride
The following data is based on the product molecular weight 426.86. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.75 mM | 3.12 mL | 15.62 mL | 31.24 mL |
| 3.75 mM | 0.62 mL | 3.12 mL | 6.25 mL |
| 7.5 mM | 0.31 mL | 1.56 mL | 3.12 mL |
| 37.5 mM | 0.06 mL | 0.31 mL | 0.62 mL |
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Product Datasheets for RS 102895 hydrochloride
References for RS 102895 hydrochloride
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for RS 102895 hydrochloride, please let us know.
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Keywords: RS 102895 hydrochloride, RS 102895 hydrochloride supplier, CCR2b, chemokine, receptor, antagonists, Chemokine, Receptors, RS102895, hydrochloride, CC, 2089, Tocris Bioscience
5 Citations for RS 102895 hydrochloride
Citations are publications that use Tocris products. Selected citations for RS 102895 hydrochloride include:
Teng et al (2017) Blocking the CCL2-CCR2 Axis Using CCL2-Neutralizing Antibody Is an Effective Therapy for Hepatocellular Cancer in a Mouse Model. Mol Cancer Ther 16 312 PMID: 27980102
Cerri et al (2016) The Chemokine CCL2 Mediates the Seizure-enhancing Effects of Systemic Inflammation. J Neurosci 36 3777 PMID: 27030762
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
Hung et al (2013) Monocyte chemoattractant protein-1 affects migration of hippocampal neural progenitors following status epilepticus in rats. J Neuroinflammation 10 11 PMID: 23339567
Do you know of a great paper that uses RS 102895 hydrochloride from Tocris? Please let us know.
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