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RS102895

Name: RS102895
Brand: TargetMol
SKU: TQ0283
Price: 37 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. TQ0283Cas No. 300815-41-2

RS102895 is a potent CCR2 antagonist (IC50: 360 nM) and shows no effect on CCR1.

RS102895

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Purity: 99.80%

Catalog No. TQ0283Cas No. 300815-41-2

RS102895 is a potent CCR2 antagonist (IC50: 360 nM) and shows no effect on CCR1.

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$37	In Stock	In Stock
5 mg	$59	In Stock	In Stock
10 mg	$97	In Stock	In Stock
25 mg	$178	In Stock	In Stock
50 mg	$268	In Stock	In Stock
100 mg	$398	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$66	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.80%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	RS102895 is a potent CCR2 antagonist (IC50: 360 nM) and shows no effect on CCR1.
Targets&IC50	CCR2:360 nM, CCR1:17800 nM, α1D-adrenoceptor (human):320 nM, 5-HT1A:470 nM, α1A-adrenoceptor:130 nM
In vitro	RS102895 also inhibits human α1a, α1d receptors, rat brain cortex 5HT1a receptor in cells with IC50s of 130, 320, 470 nM, respectively. RS102895 suppresses wild type and D284N mutant MCP-1 receptor (IC50, 550 nM and 568 nM, respectively), less potently inhibits D284A MCP-1 receptor (IC50, 1892 nM), and has no effects on E291A, E291Q, D284A/E291A or D284N/E291Q (IC50, >100,000?nM) [1]. RS102895 ameliorates the increased extracellular matrix protein expression by inhibition of CCR2 at 10 μM and obviously blocks fibronectin and type IV collagen protein expression in high glucose-stimulated mesangial cells (MCs) at 1 or 10 μM. RS102895 (10 μM) also abrogate the increased TGF-1 levels in MCs treated with MCP-1 [2].
In vivo	RS102895 at a concentration of 3 g/L progressively lowers the pain threshold in rats experiencing bone cancer pain (BCP) from days 3 to 9 post-surgery through intrathecal administration, with the threshold rising again after day 12. Additionally, RS102895 effectively alters the expression levels of NR2B, nNOS, and SIGIRR in the spinal cord.

Chemical Properties

Molecular Weight	390.4
Formula	C₂₁H₂₁F₃N₂O₂
Cas No.	300815-41-2
Smiles	O=C1OC2(C=3C(N1)=CC=CC3)CCN(CCC4=CC=C(C(F)(F)F)C=C4)CC2
Relative Density.	1.33 g/cm3 at 20℃

Storage & Solubility Information

Storage

keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (256.15 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.12 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5615 mL	12.8074 mL	25.6148 mL	128.0738 mL
5 mM	0.5123 mL	2.5615 mL	5.1230 mL	25.6148 mL
10 mM	0.2561 mL	1.2807 mL	2.5615 mL	12.8074 mL
20 mM	0.1281 mL	0.6404 mL	1.2807 mL	6.4037 mL
50 mM	0.0512 mL	0.2561 mL	0.5123 mL	2.5615 mL
100 mM	0.0256 mL	0.1281 mL	0.2561 mL	1.2807 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc