Rutaecarpine

Research use only, not for human use.

Rutaecarpine is an inhibitor of COX-2 with IC50 of 0.28 μM.

Rutaecarpine, also known as NSC 258317, is a quinazolinone alkaloid originally isolated from E. rutaecarpa that has diverse biological activities. Rutaecarpine prevented dysfunction of endothelial gap junction induced by Ox-LDL via activation of TRPV1. Rutaecarpine inhibits angiotensin II-induced proliferation in rat vascular smooth muscle cells. Rutaecarpine ameliorates hyperlipidemia and hyperglycemia in fat-fed, streptozotocin-treated rats via regulating the IRS-1/PI3K/Akt and AMPK/ACC2 signaling pathways.(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. 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.(In Vivo):Rutaecarpine showed in vivo anti-inflammatory activity on rat l-carrageenan induced paw edema by intraperitoneal administration. 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.

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. 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.

Rutaecarpine showed in vivo anti-inflammatory activity on rat l-carrageenan induced paw edema by intraperitoneal administration. 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.

Rutaecarpine | NSC 258317 | NSC-258317

Metabolic Enzyme/Protease

FXR

COX-2

Inflammation/Immunology

——

84-26-4

287.32

C18H13N3O

>98% (HPLC)

DMSO : 50 mg/mL 174.02 mM; H2O : < 0.1 mg/mL

c1cccc2c1c(=O)n1c(n2)c2c(CC1)c1c([nH]2)cccc1

8,13-dihydro-indolo[2',3':3,4]pyrido[2,1-b]quinazolin-5(7H)-one

(-20℃)

With Ice Pack

≥ 2 years