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RS102895 hydrochloride

Name: RS102895 hydrochloride
Brand: TargetMol
SKU: T12773
Price: 40 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T12773Cas No. 1173022-16-6

RS102895 hydrochloride is a potent antagonist of CCR2(IC50 of 360 nM).

RS102895 hydrochloride

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Purity: 98.95%

Catalog No. T12773Cas No. 1173022-16-6

RS102895 hydrochloride is a potent antagonist of CCR2(IC50 of 360 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$40	In Stock	In Stock
5 mg	$60	In Stock	In Stock
10 mg	$90	In Stock	In Stock
25 mg	$189	In Stock	In Stock
50 mg	$337	In Stock	In Stock
100 mg	$506	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$71	In Stock	In Stock

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

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Purity:98.95%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	RS102895 hydrochloride is a potent antagonist of CCR2(IC50 of 360 nM).
Targets&IC50	5-HT1A:470 nM, CCR1:17800 nM, CCR2:360 nM, α1D-adrenoceptor (human):320 nM, α1A-adrenoceptor:130 nM
In vitro	RS102895 hydrochloride is a potent antagonist of CCR2(IC50 : 360 nM). RS102895 inhibits human α1a and 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 with IC50 of 550 nM and 568 nM, respectively. RS102895 less potently inhibits D284A MCP-1 receptor with IC50 of 1892 nM. 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].
In vivo	Progressive decrease in pain threshold in rats with bone cancer pain (BCP) at day 3-9 after surgery via intrathecal injection caused by RS102895 (3 g/L), but the pain threshold increases after 12 days. RS102895 also potently reverses the pattern of NR2B, nNOS, and SIGIRR expression in spinal cord[3].

Chemical Properties

Molecular Weight	426.86
Formula	C₂₁H₂₂ClF₃N₂O₂
Cas No.	1173022-16-6
Smiles	Cl.FC(F)(F)c1ccc(CCN2CCC3(CC2)OC(=O)Nc2ccccc32)cc1
Relative Density.	no data available

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 28 mg/mL (65.6 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.69 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	2.3427 mL	11.7134 mL	23.4269 mL	117.1344 mL
5 mM	0.4685 mL	2.3427 mL	4.6854 mL	23.4269 mL
10 mM	0.2343 mL	1.1713 mL	2.3427 mL	11.7134 mL
20 mM	0.1171 mL	0.5857 mL	1.1713 mL	5.8567 mL
50 mM	0.0469 mL	0.2343 mL	0.4685 mL	2.3427 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