RS-102895 Hydrochloride

Catalog No.S7538 Synonyms: RS-102895 HCl

For research use only.

RS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively.

RS-102895 Hydrochloride Chemical Structure

CAS No. 1173022-16-6

Purity & Quality Control

Choose Selective CCR Inhibitors

Other CCR Products

Biological Activity

Description RS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively.
Targets
human α1a receptor [1]
(Cell-free assay)
human α1d receptor [1]
(Cell-free assay)
CCR2 [1]
(Cell-free assay)
5-HT1a receptor [1]
(Cell-free assay)
130 nM 320 nM 360 nM 470 nM
In vitro

An in vitro chemotaxis assay validates the effect of RS-102895 on leukocyte chemotaxis toward CCL2. The results suggest that increased CCL2 in SS kidneys is important in the early recruitment of leukocytes, and blockade of this recruitment by administering RS-102895 subsequently blunts the renal damage and hypertension.<sup><a class="sref" href="#s_ref">[2]</a></sup>

In vivo

The functional role of the CCL2/CCR2 pathway is tested by daily administration of CCR2 antagonist RS-102895. Blood pressure, renal leukocyte infiltration, and renal damage are evaluated. The results demonstrates that RS-102895 treatment ameliorates renal damage and hypertension after 21 days of high-salt diet. It is determined that renal leukocyte infiltration is blunted by day 3 of the high-salt diet.<sup><a class="sref" href="#s_ref">[2]</a></sup>

Protocol (from reference)

Cell Research:

<sup><a class="sref" href="#s_ref">[2]</a></sup>

  • Cell lines: peritoneal cells
  • Concentrations: 1 μM, 10 μM, 100 μM, 350 μM
  • Incubation Time: 30 min
  • Method:

    Peritoneal cells are collected and then passed through a 40-μm strainer, centrifuged, and resuspended in serum-free medium. Cells are then counted by hemocytometer, and the concentration was adjusted to 10<sup>7</sup> cells/mL. Cells are either untreated or incubated for 30 min with RS-102895 at varying concentrations, DMSO vehicle, or urine from in vivo CCR2 antagonist-treated animals.

Animal Research:

<sup><a class="sref" href="#s_ref">[2]</a></sup>

  • Animal Models: 7-wk-old male Dahl SS rats
  • Dosages: 5 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 85 mg/mL
(199.12 mM)
Water Insoluble
Ethanol '''85 mg/mL

Chemical Information

Molecular Weight 426.86
Formula

C21H22ClF3N2O2

CAS No. 1173022-16-6
Storage 3 years -20°C powder
2 years -80°C in solvent

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy RS-102895 Hydrochloride | RS-102895 Hydrochloride supplier | purchase RS-102895 Hydrochloride | RS-102895 Hydrochloride cost | RS-102895 Hydrochloride manufacturer | order RS-102895 Hydrochloride | RS-102895 Hydrochloride distributor