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.
Compound Libraries
RS 102895 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.01 | 75 |
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 |
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References
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
Keywords: RS 102895 hydrochloride, supplier, CCR2b, chemokine, receptor, antagonists, Chemokine, Receptors, RS102895, hydrochloride, Chemokine, CC, Receptors, Chemokine, CC, Receptors, Tocris Bioscience
