| Name | RS102895 |
| Description | RS102895 is a potent CCR2 antagonist (IC50: 360 nM) and shows no effect on CCR1. |
| In vitro | RS102895 also inhibits human α1a, α1d receptors, rat brain cortex 5HT1a receptor in cells with IC50s of 130, 320, 470 nM, respectively. RS102895 suppresses wild type and D284N mutant MCP-1 receptor (IC50, 550 nM and 568 nM, respectively), less potently inhibits D284A MCP-1 receptor (IC50, 1892 nM), and has no effects on E291A, E291Q, D284A/E291A or D284N/E291Q (IC50, >100,000?nM) [1]. RS102895 ameliorates the increased extracellular matrix protein expression by inhibition of CCR2 at 10 μM and obviously blocks fibronectin and type IV collagen protein expression in high glucose-stimulated mesangial cells (MCs) at 1 or 10 μM. RS102895 (10 μM) also abrogate the increased TGF-1 levels in MCs treated with MCP-1 [2]. |
| In vivo | RS102895 at a concentration of 3 g/L progressively lowers the pain threshold in rats experiencing bone cancer pain (BCP) from days 3 to 9 post-surgery through intrathecal administration, with the threshold rising again after day 12. Additionally, RS102895 effectively alters the expression levels of NR2B, nNOS, and SIGIRR in the spinal cord. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 100 mg/mL (256.15 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.12 mM), Sonication is recommended.
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| Keywords | RS-102895 | RS102895 | RS 102895 | Inhibitor | inhibit | CCR1 | CCR | CC chemokine receptor |
| Inhibitors Related | AZD2098 | MLN-3897 TFA | Artemotil | CCR2 antagonist 5 | INCB-9471 | Maraviroc | BMS-817399 | Ancriviroc | Pirfenidone | Vercirnon | PNU-177864 | CCR6 antagonist 1 |
| Related Compound Libraries | Bioactive Compound Library | Cytokine Inhibitor Library | Membrane Protein-targeted Compound Library | Chemokine Inhibitor Library | Multi-Target Compound Library | Inhibitor Library | NO PAINS Compound Library | Immuno-Oncology Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | GPCR Compound Library |
United States
