RS102895 (hydrochloride)
RS102895 (hydrochloride)
CAS: 1173022-16-6
Molecular Formula: C21H22ClF3N2O2
RS102895 (hydrochloride) - Names and Identifiers
| Name | RS102895 (hydrochloride) |
| Synonyms | RS102895 RS 102895 RS-102895 3-trihydroxybenzene RS102895 (hydrochloride) Spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one, 1'-[2-[4-(trifluoromethyl)phenyl]ethyl]-, hydrochloride |
| CAS | 1173022-16-6 |
RS102895 (hydrochloride) - Physico-chemical Properties
| Molecular Formula | C21H22ClF3N2O2 |
| Molar Mass | 426.86 |
| Solubility | DMSO: ≥ 28 mg/mL |
| Storage Condition | Inert atmosphere,Room Temperature |
| In vitro study | RS102895 hydrochloride is a potent CCR2 antagonist, with an IC 50 of 360 nM, and shows no effect on CCR1. RS102895 also inhibits human α1a and α1d receptors, rat brain cortex 5HT1a receptor in cells with IC 50 s of 130, 320, 470 nM, respectively. RS102895 suppresses wild type and D284N mutant MCP-1 receptor (IC 50 , 550 nM and 568 nM, respectively), less potently inhibits D284A MCP-1 receptor (IC 50 , 1892 nM), and has no effects on E291A, E291Q, D284A/E291A or D284N/E291Q (IC 50 , >100,000 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. |
| In vivo study | 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. |
RS102895 (hydrochloride) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.343 ml | 11.713 ml | 23.427 ml |
| 5 mM | 0.469 ml | 2.343 ml | 4.685 ml |
| 10 mM | 0.234 ml | 1.171 ml | 2.343 ml |
| 5 mM | 0.047 ml | 0.234 ml | 0.469 ml |
Last Update：2024-01-02 23:10:35
RS102895 (hydrochloride) - Reference Information
| biological activity | RS102895 hydrochloride is a potent CCR2 antagonist with an IC50 value of 360 nM and no effect on ccr1. |
Last Update：2024-04-10 22:29:15
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Product Name: RS102895 (hydrochloride) Visit Supplier Webpage Request for quotationCAS: 1173022-16-6
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Mobile: 18021002903
QQ: 3008007409
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