RS102895 free base · Synonyms: RS-102895 · RS 102895
RS102895 is a potent CCR2 antagonist.
For research use only. Not for human or veterinary use.
RS102895 structure
CAS No.: 300815-41-2
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 250 mg | USD 600.00 | BP-02266-250mg | In stock | Get quote |
| 500 mg | USD 948.00 | BP-02266-500mg | In stock | Get quote |
| 1 g | USD 1,412.00 | BP-02266-1g | In stock | Get quote |
| 5 g | Inquire | BP-02266-5g | In stock | Inquire |
| 10 g | Inquire | BP-02266-10g | In stock | Inquire |
Need another size or custom synthesis? Request a quote.
Description
RS102895 is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1.
Biological activity
RS102895 is a potent CCR2 antagonist, with IC50 value of 360 nM. RS102895 also 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 (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). 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 (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.
Identifiers
- SMILES
-
C1CN(CCC12C3=CC=CC=C3NC(=O)O2)CCC4=CC=C(C=C4)C(F)(F)F - InChIKey
-
HIDWEYPGMLIQSN-UHFFFAOYSA-N
Specifications
- MW (average)
- 390.3988
- Formula
- C21H21F3N2O2
- CAS No.
- 300815-41-2
- Physical state
- Solid
- Color
- White to off-white
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder 4℃, protect from light; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO : 175 mg/mL Ethanol : 50 mg/mL
- In vitro
- DMSO : 175 mg/mL Ethanol : 50 mg/mL