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RS102895

Catalog No. TQ0283 CAS 300815-41-2

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

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RS102895, CAS 300815-41-2

Pack Size	Availability	Price/USD
2 mg	In stock	$ 37.00
5 mg	In stock	$ 59.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 178.00
50 mg	In stock	$ 268.00
100 mg	In stock	$ 398.00
1 mL * 10 mM (in DMSO)	In stock	$ 74.00

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Purity: 99.54%

Biological Description

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Storage & Solubility Information

Description	RS102895 is a potent CCR2 antagonist (IC50: 360 nM) and shows no effect on CCR1.
Targets&IC50	5-HT1A:470 nM, CCR2:360 nM, α1D-adrenoceptor (human):320 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.

Molecular Weight	390.4
Formula	C21H21F3N2O2
CAS No.	300815-41-2

Storage

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

Solubility Information

DMSO: 15 mg/mL (38.42 mM)

References 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：

Inhibitor Library Chemokine Inhibitor Library Bioactive Compound Library Cytokine Inhibitor Library NO PAINS Compound Library Immuno-Oncology Compound Library Immunology/Inflammation Compound Library Bioactive Compounds Library Max

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Keywords

RS102895 300815-41-2 Immunology/Inflammation Microbiology/Virology CCR CC chemokine receptor Inhibitor RS 102895 RS-102895 inhibit inhibitor

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