Home GPCR & G Protein CCR antagonist - Adrenergic Receptor antagonist - 5-HT Receptor antagonist RS-102895 Hydrochloride For research use only.

RS-102895 Hydrochloride

Synonyms: RS-102895 HCl

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

RS-102895 Hydrochloride Chemical Structure

CAS: 1173022-16-6

Purity & Quality Control

Batch: S753801 DMSO] 85 mg/mL] false] Ethanol] 85 mg/mL] false] Water] Insoluble] false Purity: 99.88%
99.88

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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
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>
Cell Research 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.
In Vivo
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>
Animal Research Animal Models 7-wk-old male Dahl SS rats
Dosages 5 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 426.86 Formula

C21H22ClF3N2O2
CAS No. 1173022-16-6 SDF --
Smiles Cl.FC(F)(F)C1=CC=C(CCN2CCC3(CC2)OC(=O)NC4=CC=CC=C34)C=C1
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 85 mg/mL ( (199.12 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 85 mg/mL

Water : Insoluble


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In vivo
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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.

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