Name | 6-methyl-1'-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethyl]spiro[3,1-benzoxazine-4,4'-piperidin]-2(1H)-one |
Synonyms | RS504393 RS 504393 RS-504393 6-Methyl-1'-[2-(5-Methyl-2-phenyl-4-oxazolyl)ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidi 6-Methyl-1'-(2-(5-methyl-2-phenyloxazol-4-yl)ethyl)spiro-[benzo[d][1,3]oxazine-4,4'-piperidin] 6-Methyl-1'-(2-(5-methyl-2-phenyloxazol-4-yl)ethyl)spiro-[benzo[d][1,3]oxazine-4,4'-piperidin]-2( 6-Methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one 6-Methyl-1'-(2-(5-Methyl-2-phenyloxazol-4-yl)ethyl)spiro[benzo[d][1,3]oxazine-4,4'-piperidin]-2(1H)-one 6-Methyl-1'-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethyl]spiro[3,1-benzoxazine-4,4'-piperidin]-2(1H)-one 6-methyl-1'-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethyl]spiro[3,1-benzoxazine-4,4'-piperidin]-2(1H)-one Spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one, 6-Methyl-1'-[2-(5-Methyl-2-phenyl-4-oxazolyl)ethyl]- Spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one, 6-methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]- |
CAS | 300816-15-3 |
InChI | InChI=1/C25H27N3O3/c1-17-8-9-22-20(16-17)25(31-24(29)27-22)11-14-28(15-12-25)13-10-21-18(2)30-23(26-21)19-6-4-3-5-7-19/h3-9,16H,10-15H2,1-2H3,(H,27,29) |
Molecular Formula | C25H27N3O3 |
Molar Mass | 417.5 |
Density | 1.28 |
Solubility | DMSO: soluble1mg/mL, clear (warmed) |
Appearance | powder |
Color | white to beige |
Storage Condition | 2-8°C |
Refractive Index | 1.645 |
MDL | MFCD09038564 |
In vitro study | RS 504393 inhibits the MCP-1-induced chemotaxis with an IC 50 of 330 nM. RS 504393 treatment suppresses allergen induced β-hexosaminidase release significantly. Without allergen priming, MCP-1 induces mast cell degranulation, which is completely suppressed by RS 504393. |
In vivo study | RS504393 (0.3-3 μg) with CCL2 progressively blocks thermal hyperalgesia dose-dependently in mice. RS 504393 (5mg/kg, i.v.) supresses the elevated numbers of leukocytes and increased total protein content in BALF induced by The LPS. RS504393 significantly down regulates the LPS-induced elevation of IL-1β, PAI-1 mRNA and protein expressions. RS504393 significantly suppresses induced lung edema, protein-rich fluid, polymorphonuclear accumulation and bronchial wall thickening induced by LPS. RS-504393 significantly reduces renal pathology, especially the extensive interstitial fibrosis mediated by decrease in type I collagen synthesis in a UUO model. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.395 ml | 11.976 ml | 23.952 ml |
5 mM | 0.479 ml | 2.395 ml | 4.79 ml |
10 mM | 0.24 ml | 1.198 ml | 2.395 ml |
5 mM | 0.048 ml | 0.24 ml | 0.479 ml |
biological activity | RS 504393 is a selective CCR2 antagonist that acts on human recombinant CCR2 and CCR1 receptors with IC50 values of 89 nM and> 100 μM respectively. |
target | CCR2 89 nM (IC 50 ) Human α 1a receptor 72 nM (IC 50 ) Human α 1d receptor 460 nM (IC 50 ) 5HT-1a receptor 1070 nM (IC 50 ) |
in vitro study | RS 504393 inhibits the MCP-1-induced chemotaxis with an IC 50 of 330 nM. RS 504393 treatment suppresses allergen induced β-hexosaminidase release significantly. Without allergen priming, MCP-1 induces mast cell degranulation, which is completely suppressed by RS 504393. |
in vivo study | RS504393 (0.3-3 μg) with CCL2 progressively blocks thermal hyperalgesia dose-dependently in ice. RS 504393 (5 mg/kg, I. v.) supresses the elevated numbers of leukocytes and increased total protein content in BALF induced by The LPS. RS504393 significantly down regulates the LPS-induced elevation of IL-1β, PAI-1 mRNA and protein expressions. RS504393 significantly suppresses induced lung edema, protein-rich fluid, polymorphonuclear accumulation and bronchial wall thickening induced by LPS. RS-504393 significantly reduces pathology, especially the extensive interstitial fibrosis mediated by decrease in type I collagen synthesis in a UUO model. |