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RS102895
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
RS102895图片
CAS NO:300815-41-2
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
RS102895 是一种CCR2拮抗剂,IC50值为 360 nM。

产品描述

RS102895 is a potent CCR2 antagonist (IC50: 360 nM) and shows no effect on CCR1.

体外活性

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].

体内活性

RS102895 (3 g/L) causes a 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 the spinal cord [3].

Cas No.

300815-41-2

分子式

C21H21F3N2O2

分子量

390.4

储存和溶解度

DMSO:15 mg/mL (38.42 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years