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RS102895 hydrochloride

RS102895 hydrochloride
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Purity:99.7%
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RS102895 hydrochloride

Catalog No. T12773Cas No. 1173022-16-6
RS102895 hydrochloride is a potent antagonist of CCR2(IC50 of 360 nM).
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Pack SizePriceAvailabilityQuantity
2 mg$40In Stock
5 mg$60In Stock
10 mg$90In Stock
25 mg$189In Stock
50 mg$337In Stock
100 mg$506In Stock
1 mL x 10 mM (in DMSO)$71In Stock
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Product Introduction

Bioactivity
Description
RS102895 hydrochloride is a potent antagonist of CCR2(IC50 of 360 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 Weight426.86
FormulaC21H22ClF3N2O2
Cas No.1173022-16-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 28 mg/mL (65.60 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3427 mL11.7134 mL23.4269 mL117.1344 mL
5 mM0.4685 mL2.3427 mL4.6854 mL23.4269 mL
10 mM0.2343 mL1.1713 mL2.3427 mL11.7134 mL
20 mM0.1171 mL0.5857 mL1.1713 mL5.8567 mL
50 mM0.0469 mL0.2343 mL0.4685 mL2.3427 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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