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RS102895 hydrochloride

CAS No. : 1173022-16-6

MCE 站：RS102895 hydrochloride

产品活性：RS102895 hydrochloride 是一种有效的 CCR2 拮抗剂，IC₅₀ 值为 360 nM，对 CCR1 无作用。

研究领域：GPCR/G Protein  |  Immunology/Inflammation

作用靶点：CCR

In Vitro: RS102895 hydrochloride is a potent CCR2 antagonist, with an IC₅₀ 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 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). 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: 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.

相关产品：Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Immunology/Inflammation Compound Library  |  Small Molecule Immuno-Oncology Compound Library  |  Endocrinology Compound Library  |  Pirfenidone  |  Maraviroc  |  RS 504393  |  INCB3344  |  PF-4136309  |  Bindarit  |  BX471  |  TAK-779  |  AZ084  |  CCR6 inhibitor 1  |  CCR2-RA-[R]  |  7,4'-Dihydroxyflavone  |  TAK-220  |  INCB 3284  |  CCR2 antagonist 4 hydrochloride  |  J-113863  |  DAPTA  |  Vicriviroc maleate  |  K777  |  LMD-009  |  SB297006  |  ZK756326 dihydrochloride  |  CCR2 antagonist 3  |  AZD2423  |  CCR2 antagonist 1  |  RS102895  |  YM022

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