Name | Rutaecarpine |
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Synonyms |
ruteacarpine
Rutecarpine MFCD00210551 Indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5(7H)-one, 8,13-dihydro- RUTECARPINE 95+ 8,13-Dihydroindolo[2',3':3,4]pyrido[2,1-b]quinazolin-5(7H)-one |
Description | Rutaecarpine, an alkaloid of Evodia rutaecarpa, is an inhibitor of COX-2 with an IC50 value of 0.28 μM. |
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Related Catalog | |
Target |
COX-2:0.28 μM (IC50, in BMMC) COX-1:8.7 μM (IC50, in BMMC) |
In Vitro | Rutaecarpine has shown a variety of intriguing biological properties such as anti-thrombotic, anticancer, anti-inflammatory and analgesic, anti-obesity and thermoregulatory, vasorelaxing activity, as well as effects on the cardiovascular and endocrine systems[2]. Rutaecarpine inhibits COX-2 and COX-1 dependent phases of PGD2 generation in BMMC in a concentration-dependent manner with an IC50 of 0.28 μM and 8.7 μM, respectively. It inhibits COX-2-dependent conversion of exogenous arachidonic acid to PGE2 in a dose-dependent manner by the COX-2-transfected HEK293 cells[1]. |
In Vivo | Rutaecarpine showed in vivo anti-inflammatory activity on rat l-carrageenan induced paw edema by intraperitoneal administration[1]. Rutaecarpine significantly decreases the number of antibody-forming cells and causes weight decrease in spleen in a dose-dependent manner. In addition, rutaecarpine administered mice exhibit reduced splenic cellularity, decreased numbers of total T cells, CD4+ cells, CD8+ cells, and B cells in spleen. IL-2, interferon and IL-10 mRNA expressions are suppressed significantly by rutaecarpine treatment. The number of CD4+IL-2+ cells is reduced significantly following administration of mice with rutaecarpine[3]. |
Cell Assay | Rutaecarpine is dissolved in DMSO and diluted with appropriate medium before use. COX-1 and COX-2 cDNA-transfected HEK293 cells are prepared. For measuring inhibitory activity on COX-1 and COX-2 by rutaecarpine, cells in 1 mL of culture medium are seeded into each well of 24-well. After culture for 4 days, the supernatants are removed and 250 mL of fresh medium is added to the cells with or without rutaecarpine. After preincubation for 5 h at 37°C, the cells are further incubated at 37°C for 30 min with 50 mM arachidonic acid. All reactions are stopped by centrifugation at 120 g at 4°C for 5 min. Concentrations of PGE2 in the supernatant are measured[1]. |
Animal Admin | Rats: Rutaecarpine is dissolved in 0.1% carboxymethyl cellulose and diluted with appropriate medium before use. Male Splague-Dawley (SD) rats (180-220 g) are used in the study. Rutaecarpine administered intraperitoneally and, 1 h later, l-carrageenan solution is injected to right hind paw of rats. Paw volumes are measured using plethysmometer 5 h after l-carrageenan injection[1]. Mice: For the antibody response to SRBCs, rutaecarpine is administered at a single dose of 10 mg/kg, 20 mg/kg, 40 mg/kg or 80 mg/kg in 10 mL of 1% povidone solution intravenously. Control animals are given 1% povidone solution at 10 mL/kg. Specific pathogen-free female BALB/c mice are used in the study[3]. |
References |
[2]. Lee SH, et al. Progress in the studies on rutaecarpine. Molecules. 2008 Feb 6;13(2):272-300. |
Density | 1.5±0.1 g/cm3 |
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Boiling Point | 550.1±60.0 °C at 760 mmHg |
Melting Point | 259.5 - 260ºC |
Molecular Formula | C18H13N3O |
Molecular Weight | 287.315 |
Flash Point | 286.5±32.9 °C |
Exact Mass | 287.105865 |
PSA | 50.68000 |
LogP | 2.03 |
Vapour Pressure | 0.0±1.5 mmHg at 25°C |
Index of Refraction | 1.792 |
Storage condition | 2-8°C |
Water Solubility | DMSO: 18 mg/mL clear yellow solution, soluble |
Personal Protective Equipment | Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges |
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Hazard Codes | T:Toxic; |
Risk Phrases | R25 |
Safety Phrases | S45 |
RIDADR | UN 2811 6.1/PG 3 |
WGK Germany | 3 |
Packaging Group | III |
Hazard Class | 6.1 |
HS Code | 2933990090 |
Precursor 5 | |
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DownStream 3 | |
HS Code | 2933990090 |
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Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |