Home GPCR & G Protein CCR antagonist - Adrenergic Receptor antagonist - 5-HT Receptor antagonist RS-102895 Hydrochloride

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RS-102895 Hydrochloride CCR antagonist

Cat.No.S7538

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 CCR antagonist Chemical Structure

Chemical Structure

Molecular Weight: 426.86

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 426.86 Formula

C21H22ClF3N2O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1173022-16-6 -- Storage of Stock Solutions

Synonyms RS-102895 HCl Smiles Cl.FC(F)(F)C1=CC=C(CCN2CCC3(CC2)OC(=O)NC4=CC=CC=C34)C=C1

Solubility

In vitro
Batch:

DMSO : 85 mg/mL (199.12 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 85 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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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.
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Mechanism of Action

Targets/IC50/Ki
human α1a receptor [1]
(Cell-free assay)
130 nM
human α1d receptor [1]
(Cell-free assay)
320 nM
CCR2 [1]
(Cell-free assay)
360 nM
5-HT1a receptor [1]
(Cell-free assay)
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>
References

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