[CAS NO. 1173022-16-6] RS102895hydrochloride

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PRODUCTS SPECIFICATIONS [1173022-16-6]

Catalog

HY-18611

Brand

MCE

CAS

1173022-16-6

DESCRIPTION [1173022-16-6]

Overview

MDL	MFCD08703093
Molecular Weight	426.86
Molecular Formula	C21H22ClF3N2O2
SMILES	[H]Cl.O=C1NC2=CC=CC=C2C3(CCN(CCC4=CC=C(C(F)(F)F)C=C4)CC3)O1

For research use only. We do not sell to patients.

14 Publications Citing Use of MCE

Summary

RS102895 hydrochloride is a potent CCR2 antagonist, with an IC ₅₀ of 360 nM, and shows no effect on CCR1 .

IC50 & Target

CCR2

360 nM (IC ₅₀ )

CCR1

17800 nM (IC ₅₀ )

Human α _1a receptor

130 nM (IC ₅₀ )

Human α _1d receptor

320 nM (IC ₅₀ )

5HT-1a receptor

470 nM (IC ₅₀ )

In Vitro

RS102895 hydrochloride is a potent CCR2 antagonist, with an IC ₅₀ of 360 nM, and shows no effect on CCR1. RS102895 also inhibits human α1a and α1d receptors, rat brain cortex 5HT1a receptor in cells with IC ₅₀ s of 130, 320, 470 nM, respectively. RS102895 suppresses wild type and D284N mutant MCP-1 receptor (IC ₅₀ , 550 nM and 568 nM, respectively), less potently inhibits D284A MCP-1 receptor (IC ₅₀ , 1892 nM), and has no effects on E291A, E291Q, D284A/E291A or D284N/E291Q (IC ₅₀ , >100,000 nM) ^[1] . RS102895 ameliorates the increased extracellular matrix (ECM) protein expression by inhibition of CCR2 at 10 μM, and obviously blocks fibronectin and type IV collagen protein expression in high glucose (HG)-stimulated mesangial cells (MCs) at 1 or 10 μM. RS102895 (10 μM) also abrogates the increased TGF-1 levels in MCs treated with MCP-1 ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

RS102895 (3 g/L) causes progressive decrease in pain threshold in rats with bone cancer pain (BCP) at day 3-9 after surgery via intrathecal injection, but the pain threshold increases after 12 days. RS102895 also potently reverses the pattern of NR2B, nNOS, and SIGIRR expression in spinal cord ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 41.67 mg/mL ( 97.62 mM ; ultrasonic and warming and heat to 60°C)

H ₂ O : 5 mg/mL ( 11.71 mM ; ultrasonic and adjust pH to 12 with NaOH)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3427 mL	11.7134 mL	23.4269 mL
5 mM	0.4685 mL	2.3427 mL	4.6854 mL
10 mM	0.2343 mL	1.1713 mL	2.3427 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.87 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.87 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.87 mM); Clear solution

* All of the co-solvents are available by MCE.