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CCR2-RA-[R]

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Purity:99.65%

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COA HNMR HPLC

CCR2-RA-[R]

Catalog No. T14900Cas No. 512177-83-2

CCR2-RA-[R] is a C-C chemokine receptor type 2 (CCR2) allosteric antagonist (IC50: 103 nM).

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Pack Size	Price	Availability
2 mg	$39	In Stock
5 mg	$64	In Stock
10 mg	$97	In Stock
25 mg	$197	In Stock
50 mg	$320	In Stock
100 mg	$441	In Stock
1 mL x 10 mM (in DMSO)	$70	In Stock

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Product Introduction

Bioactivity

Description	CCR2-RA-[R] is a C-C chemokine receptor type 2 (CCR2) allosteric antagonist (IC50: 103 nM).
Targets&IC50	CCR2:103 nM (in U2OS-CCR2 cells)
In vitro	CCR2-RA-[R] inhibits CCR2 non-competitively by blocking activation-associated conformational changes and formation of the G protein-binding interface. CCR2-RA-[R] displaces [125I]CCL2 from CCR2 with an pIC50 value of 6.1. The pKD of CCR2-RA-[R] for CCR2 and CCR5 is 8.8±0.1 and 7.0±0.1, respectively[2]. The chemokine receptor CCR2 is a G protein-coupled receptor that is involved in many diseases characterized by chronic inflammation, and therefore a large variety of CCR2 small molecule antagonists has been developed. The binding pocket of CCR2-RA-[R] is highly enclosed and possesses a balanced combination of hydrophobic and polar features, all of which favors pocket “druggability”[3].

Chemical Properties

Molecular Weight	351.8
Formula	C18H19ClFNO3
Cas No.	512177-83-2

Storage & Solubility Information

Storage

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

Solubility Information

H2O: < 0.1 mg/mL (insoluble)

DMSO: 125 mg/mL (355.32 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.8425 mL	14.2126 mL	28.4252 mL	142.1262 mL
5 mM	0.5685 mL	2.8425 mL	5.6850 mL	28.4252 mL
10 mM	0.2843 mL	1.4213 mL	2.8425 mL	14.2126 mL
20 mM	0.1421 mL	0.7106 mL	1.4213 mL	7.1063 mL
50 mM	0.0569 mL	0.2843 mL	0.5685 mL	2.8425 mL
100 mM	0.0284 mL	0.1421 mL	0.2843 mL	1.4213 mL

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In Vivo Formulation Calculator (Clear solution)

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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