RS-102895 Hydrochloride

Catalog No.S7538 Batch:S753801

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Technical Data

Formula

C21H22ClF3N2O2
Molecular Weight 426.86 CAS No. 1173022-16-6
Solubility (25°C)* In vitro DMSO 85 mg/mL (199.12 mM)
Ethanol 85 mg/mL (199.12 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
4.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 90 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:

<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 Study:

<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.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.