RS102895 HCl

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Chemical Structure| 1173022-16-6 同义名 : RS 102895 (hydrochloride);RS-102895 Hydrochloride
CAS号 : 1173022-16-6
货号 : A123914
分子式 : C21H22ClF3N2O2
纯度 : 99%
分子量 : 426.86
MDL号 : MFCD08703093
存储条件：

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(81.99 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 5%DMSO+H2O 1 mg/mL clear

生物活性
描述 RS102895 hydrochloride acts as a strong antagonist of CCR2, demonstrating an IC50 value of 360 nM, while exhibiting no influence on CCR1. This compound further exerts inhibitory effects on human α1a and α1d receptors, along with the 5HT1a receptor in rat brain cortex cells, showcasing IC50 values of 130, 320, and 470 nM, respectively. It effectively diminishes activity in both the wild type and D284N variant of the MCP-1 receptor, with IC50 figures of 550 nM and 568 nM, respectively, and exhibits a weaker inhibition against the D284A variant of MCP-1 receptor (IC50 of 1892 nM). It displays no impact on the E291A, E291Q, D284A/E291A, or D284N/E291Q variants of MCP-1 receptor (IC50 exceeding 100,000 nM)[1]. By blocking CCR2 with a concentration of 10 μM, RS102895 reduces the upregulation of extracellular matrix (ECM) protein expression and significantly prevents the expression of fibronectin and type IV collagen proteins in mesangial cells (MCs) stimulated by high glucose (HG) at concentrations of 1 or 10 μM. Furthermore, a 10 μM dose of RS102895 also lowers the enhanced levels of TGF-1 in MCs treated with MCP-1[2].
作用机制 RS-102895 hydrochloride prevents MCP-1 from binding to CCR2 by occupying the same binding-site, the inter-helical bundle region on the extracellular side of CCR2 receptor.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.71mL

2.34mL

1.17mL

23.43mL

4.69mL

2.34mL
参考文献

[1]Mirzadegan T, et al. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle. J Biol Chem. 2000 Aug 18;275(33):25562-71.

[2]Park J, et al. MCP-1/CCR2 system is involved in high glucose-induced fibronectin and type IV collagen expression in cultured mesangial cells. Am J Physiol Renal Physiol. 2008 Sep;295(3):F749-57.

[3]Ren F, et al. Analgesic Effect of Intrathecal Administration of Chemokine Receptor CCR2 Antagonist is Related to Change in Spinal NR2B, nNOS, and SIGIRR Expression in Rat with Bone Cancer Pain. Cell Biochem Biophys. 2015 Jun;72(2):611-6.