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[CAS NO. 1173022-16-6] RS102895hydrochloride
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-18611 |
| Brand: | MCE |
| CAS: | 1173022-16-6 |
Overview
| MDL | MFCD08703093 |
|---|---|
| Molecular Weight | 426.86 |
| Molecular Formula | C21H22ClF3N2O2 |
| SMILES | [H]Cl.O=C1NC2=CC=CC=C2C3(CCN(CCC4=CC=C(C(F)(F)F)C=C4)CC3)O1 |
14 Publications Citing Use of MCE
- [1]Theranostics. 2020 Apr 27;10(13):5687-5703
- [2]J Adv Res. 2020 Jul 22;28:231-243.
- [3]Cell Death Dis. 2022 Feb 17;13(2):158.
- [4]Hum Reprod. 2019 Apr 1;34(4):646-658.
- [5]J Eur Acad Dermatol Venereol. 2020 Apr;34(4):862-872.
- [6]Liver Int. 2022 Sep 27.
- [7]Stem Cell Res Ther. 2021 Jul 2;12(1):378.
- [8]Int Immunopharmacol. 2023 Feb.
- [9]Life Sci. 2020 Nov 15;261:118360.
- [10]Exp Cell Res. 2020 Nov 1;396(1):112289.
- [11]Eur J Pharmacol. 2021, 174165.
- [12]Mol Med Rep. 2017 Sep;16(3):3387-3394.
- [13]J Interferon Cytokine Res. 2020 May;40(5):245-253.
- [14]J Interferon Cytokine Res. 2019 Apr;39(4):224-232.
Summary
IC50 & Target
|
CCR2 360 nM (IC 50 ) |
CCR1 17800 nM (IC 50 ) |
Human α 1a receptor 130 nM (IC 50 ) |
Human α 1d receptor 320 nM (IC 50 ) |
5HT-1a receptor 470 nM (IC 50 ) |
In Vitro
RS102895 hydrochloride is a potent CCR2 antagonist, with an IC 50 of 360 nM, and shows no effect on CCR1. RS102895 also inhibits human α1a and α1d receptors, rat brain cortex 5HT1a receptor in cells with IC 50 s of 130, 320, 470 nM, respectively. RS102895 suppresses wild type and D284N mutant MCP-1 receptor (IC 50 , 550 nM and 568 nM, respectively), less potently inhibits D284A MCP-1 receptor (IC 50 , 1892 nM), and has no effects on E291A, E291Q, D284A/E291A or D284N/E291Q (IC 50 , >100,000 nM) [1] . 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
RS102895 (3 g/L) causes progressive decrease in pain threshold in rats with bone cancer pain (BCP) at day 3-9 after surgery via intrathecal injection, but the pain threshold increases after 12 days. RS102895 also potently reverses the pattern of NR2B, nNOS, and SIGIRR expression in spinal cord [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 41.67 mg/mL ( 97.62 mM ; ultrasonic and warming and heat to 60°C)
H 2 O : 5 mg/mL ( 11.71 mM ; ultrasonic and adjust pH to 12 with NaOH)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3427 mL | 11.7134 mL | 23.4269 mL |
| 5 mM | 0.4685 mL | 2.3427 mL | 4.6854 mL |
| 10 mM | 0.2343 mL | 1.1713 mL | 2.3427 mL |
References
- [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.
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