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RS102895 hydrochloride

Catalog No. T12773   CAS 1173022-16-6

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

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RS102895 hydrochloride Chemical Structure
RS102895 hydrochloride, CAS 1173022-16-6
Pack Size Availability Price/USD Quantity
2 mg In stock $ 40.00
5 mg In stock $ 60.00
10 mg In stock $ 90.00
25 mg In stock $ 189.00
50 mg In stock $ 337.00
100 mg In stock $ 506.00
1 mL * 10 mM (in DMSO) In stock $ 71.00
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Purity: 99.7%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description RS102895 hydrochloride is a potent antagonist of CCR2(IC50 of 360 nM).
Targets&IC50 5-HT1A:470 nM, CCR2:360 nM, CCR1:17800 nM, Human α1d receptor:320 nM, Human α1a receptor: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].
Molecular Weight 426.86
Formula C21H22ClF3N2O2
CAS No. 1173022-16-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 28 mg/mL (65.60 mM)

TargetMolReferences and Literature

1. Mirzadegan T, et al. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle. J Biol Chem. 2000 Aug 18;275(33):25562-71. 2. Park J, et al. MCP-1/CCR2 system is involved in high glucose-induced fibronectin and type IV collagen expression in cultured mesangial cells. Am J Physiol Renal Physiol. 2008 Sep;295(3):F749-57. 3. Ren F, et al. Analgesic Effect of Intrathecal Administration of Chemokine Receptor CCR2 Antagonist is Related to Change in Spinal NR2B, nNOS, and SIGIRR Expression in Rat with Bone Cancer Pain. Cell Biochem Biophys. 2015 Jun;72(2):611-6.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Neuronal Signaling Compound Library Inhibitor Library Cytokine Inhibitor Library Bioactive Compounds Library Max Neurotransmitter Receptor Compound Library Anti-Parkinson's Disease Compound Library Anti-Cancer Compound Library GPCR Compound Library Bioactive Compound Library

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Keywords

RS102895 hydrochloride 1173022-16-6 GPCR/G Protein Immunology/Inflammation Microbiology/Virology Neuroscience Others 5-HT Receptor CCR RS-102895 hydrochloride CC chemokine receptor Inhibitor RS-102895 inhibit RS 102895 Hydrochloride RS-102895 Hydrochloride RS 102895 RS102895 Hydrochloride RS102895 inhibitor

 

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