|
|
| | RS-102895 hydrochloride Basic information |
| Product Name: | RS-102895 hydrochloride | | Synonyms: | Spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one, 1'-[2-[4-(trifluoromethyl)phenyl]ethyl]-, hydrochloride;RS-102895;RS 102895;RS102895;Spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one, 1'-[2-[4-(trifluoromethyl)phenyl]ethyl]-, hydrochloride (1:1);3-trihydroxybenzene;1'-(4-(Trifluoromethyl)phenethyl)spiro[benzo[d][1,3]oxazine-4,4'-piperidin]-2(1H)-one hydrochloride;RS 102895 hydrochloride, CCR2 receptor antagonist;RS102895 hydrochloride, 10 mM in DMSO;RS-102895 Hydrochloride ，S7538 | | CAS: | 1173022-16-6 | | MF: | C21H22ClF3N2O2 | | MW: | 426.86 | | EINECS: | | | Product Categories: | | | Mol File: | 1173022-16-6.mol |  |
| | RS-102895 hydrochloride Chemical Properties |
| storage temp. | Inert atmosphere,Room Temperature | | solubility | DMF: 25 mg/ml; DMSO: 30 mg/ml; DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml; Ethanol: 2 mg/ml | | form | Powder | | color | White to off-white |
| | RS-102895 hydrochloride Usage And Synthesis |
| Description | The chemokine CCL2, also known as monocyte chemotactic protein-1 (MCP-1), stimulates leukocyte chemotaxis to sites of inflammation via signaling through the MCP-1 receptor, CCR2. RS 102895 is a spiropiperidine compound that acts as a CCR2 antagonist (IC50 = 0.36 μM). It inhibits the related CCR1 receptor with an IC50 value of 17.8 μM and inhibits adrenergic α1a, α1d, and 5HT1A receptors with IC50 values of 0.13, 0.32, and 47 μM, respectively. RS 102895 prevents chemotaxis of THP-1 cells (IC50 = 1.7 μM) when MCP-1 is presented as a chemoattractant. | | Uses | RS 102895 Hydrochloride is used as a leukocyte infiltrate marker for rosacea diagnosis. | | in vivo | RS102895 (3 g/L) causes progressive decrease in pain threshold in rats with bone cancer pain (BCP) at day 3-9 after surgery via intrathecal injection, but the pain threshold increases after 12 days. RS102895 also potently reverses the pattern of NR2B, nNOS, and SIGIRR expression in spinal cord[3]. | | IC 50 | CCR2: 360 nM (IC50); CCR1: 17800 nM (IC50); Human α1a receptor: 130 nM (IC50); Human α1d receptor: 320 nM (IC50); 5HT-1a receptor: 470 nM (IC50) | | storage | Desiccate at RT | | References | [1] T MIRZADEGAN. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle.[J]. The Journal of Biological Chemistry, 2000, 275 33: 25562-25571. DOI: 10.1074/jbc.m000692200 |
| | RS-102895 hydrochloride Preparation Products And Raw materials |
|