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RS102895
🥰Excellent
Catalog No. TQ0283Cas No. 300815-41-2
RS102895 is a potent CCR2 antagonist (IC50: 360 nM) and shows no effect on CCR1.
RS102895
🥰Excellent
Purity: 99.54%
Catalog No. TQ0283Cas No. 300815-41-2
RS102895 is a potent CCR2 antagonist (IC50: 360 nM) and shows no effect on CCR1.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $37 | In Stock | |
| 5 mg | $59 | In Stock | |
| 10 mg | $97 | In Stock | |
| 25 mg | $178 | In Stock | |
| 50 mg | $268 | In Stock | |
| 100 mg | $398 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $66 | In Stock |
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Purity:99.54%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | RS102895 is a potent CCR2 antagonist (IC50: 360 nM) and shows no effect on CCR1. |
| Targets&IC50 | α1A-adrenoceptor:130 nM, α1D-adrenoceptor (human):320 nM, CCR2:360 nM, 5-HT1A:470 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 |
| Smiles | O=C1OC2(C=3C(N1)=CC=CC3)CCN(CCC4=CC=C(C(F)(F)F)C=C4)CC2 |
| Relative Density. | 1.33 g/cm3 at 20℃ |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 15 mg/mL (38.42 mM) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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