| Name | RS102895 hydrochloride |
| Description | RS102895 hydrochloride is a potent antagonist of CCR2(IC50 of 360 nM). |
| In vitro | RS102895 hydrochloride is a potent antagonist of CCR2(IC50 : 360 nM). RS102895 inhibits human α1a and 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 with IC50 of 550 nM and 568 nM, respectively. RS102895 less potently inhibits D284A MCP-1 receptor with IC50 of 1892 nM. RS102895 ameliorates the increased extracellular matrix (ECM) protein expression by inhibition of CCR2 at 10 μM, and obviously blocks fibronectin and type IV collagen protein expression in high glucose (HG)-stimulated mesangial cells (MCs) at 1 or 10 μM. RS102895 (10 μM) also abrogates the increased TGF-1 levels in MCs treated with MCP-1[2]. |
| In vivo | Progressive decrease in pain threshold in rats with bone cancer pain (BCP) at day 3-9 after surgery via intrathecal injection caused by RS102895 (3 g/L), but the pain threshold increases after 12 days. RS102895 also potently reverses the pattern of NR2B, nNOS, and SIGIRR expression in spinal cord[3]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 28 mg/mL (65.6 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.69 mM), Sonication is recommended.
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| Keywords | RS-102895 hydrochloride | RS102895 hydrochloride | RS-102895 | RS102895 | RS 102895 Hydrochloride | RS 102895 | Inhibitor | inhibit | Human α1d receptor | Human α1a receptor | CCR2 | CCR1 | CCR | CC chemokine receptor | 5HTReceptor | 5HT-1a receptor | 5-HT1A | 5HT Receptor |
| Inhibitors Related | Alverine citrate | Dapoxetine hydrochloride | Cefaclor monohydrate | Clozapine N-Oxide | 1,8-Cineole | Dopamine hydrochloride | Cloperastine hydrochloride | Pirfenidone | Mianserin hydrochloride | Trazodone hydrochloride | Cinchonidine | Doxepin hydrochloride |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Pain-Related Compound Library | Cytokine Inhibitor Library | Membrane Protein-targeted Compound Library | Neurotransmitter Receptor Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library | Serotonin Receptor-Targeted Compound Library |
United States
