RS 102895

Name	RS 102895
Synonyms	RS 102895 RS 102895 HYDROCHLORIDE 1'-(4-(trifluoromethyl)phenethyl)spiro[benzo[d][1,3]oxazine-4,4'-piperidin]-2(1H)-one 1'-[2-[4-(trifluoromethyl)phenyl]ethyl]-spiro[4h-3,1-benzoxazine-4,4'-peperidin]-2(1h)-one Spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one, 1'-[2-[4-(trifluoromethyl)phenyl]ethyl]- 1'-(4-(TrifluoroMethyl)phenethyl)spiro[benzo[d][1,3]oxazine-4,4'-piperidin]-2(1H)-one hydrochloride 1'-[2-[4-(trifluoromethyl)phenyl]ethyl]spiro[1H-3,1-benzoxazine-4,4'-piperidine]-2-one,hydrochloride 1'-[2-[4-(TRIFLUOROMETHYL)PHENYL]ETHYL]-SPIRO[4H-3,1-BENZOXAZINE-4,4'-PIPERIDIN]-2(1H)-ONE HYDROCHLORIDE
CAS	300815-41-2

Molecular Formula	C21H21F3N2O2
Molar Mass	390.4
Density	1.33±0.1 g/cm3 (20 ºC 760 Torr)
Boling Point	446.1±45.0 °C(Predicted)
Solubility	DMSO: 18mg/mL, clear, colorless
Appearance	powder
Color	white
pKa	13.46±0.20(Predicted)
Storage Condition	Desiccate at RT
In vitro study	RS102895 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.

Safety Description	S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes.
WGK Germany	3

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Product Name: RS 102895 Visit Supplier Webpage Request for quotation
CAS: 300815-41-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

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RS 102895

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