Rutaecarpine (Synonyms: NSC 258317) |
Catalog No.GN10039
One-Click Copy Product Info
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Rutaecarpine es un alacaloide de indolopiridoquinazolina aislado de Evodia rutaecarpa y conocido por inhibir la COX-2 con un IC50 de 0.28μM a nivel celular.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 84-26-4
Sample solution is provided at 25 µL, 10mM.
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Rutaecarpine es un alacaloide de indolopiridoquinazolina aislado de Evodia rutaecarpa y conocido por inhibir la COX-2 con un IC50 de 0.28μM a nivel celular[1]. Rutaecarpine exhibe varios efectos farmacológicos, como efectos antiinflamatorios[2], antiapoptóticos y antioxidantes[3]. Rutaecarpine juega un papel crítico en enfermedades cardiovasculares[4], del sistema nervioso, inflamatorias y tumorales[5].
Rutaecarpine a concentraciones de 10µM durante 24h atenuó efectivamente la apoptosis de condrocitos inducida por IL?1β, la senescencia y el deterioro de la autofagia en los condrocitos[6]. En las células HepG2, Rutaecarpine a concentraciones de 40µM durante 24h aumenta p-GSK-3b y p-AMPK, y disminuye la expresión de G6Pase[7].
Rutaecarpine (20mg/kg, administración intragástrica, diaria durante 9 días) inhibió el estrés oxidativo en ratones inducidos por NTG y mejora la migraña mediante la activación del sistema antioxidante Nrf2 a través de la vía PTEN/PGK1[8]. Rutaecarpine (10mg/kg, 20mg/kg, 40mg/kg) disminuyó significativamente el número de células formadoras de anticuerpos y causó una disminución del peso en el bazo del ratón de una manera dependiente de la dosis[9].
References:
[1]. Moon TC, Murakami M, Kudo I, et al. A new class of COX-2 inhibitor, rutaecarpine from Evodia rutaecarpa. Inflamm Res. 1999 Dec;48(12):621-5. doi: 10.1007/s000110050512. PMID: 10669112.
[2]. Jayakumar T, Lin KC, Chang CC, et al. Targeting MAPK/NF-κB Pathways in Anti-Inflammatory Potential of Rutaecarpine: Impact on Src/FAK-Mediated Macrophage Migration. Int J Mol Sci. 2021 Dec 22;23(1):92. doi: 10.3390/ijms23010092. PMID: 35008520; PMCID: PMC8745017.
[3]. Choi JH, Jin SW, Lee GH, et al. Rutaecarpine Protects against Acetaminophen-Induced Acute Liver Injury in Mice by Activating Antioxidant Enzymes. Antioxidants (Basel). 2021 Jan 10;10(1):86. doi: 10.3390/antiox10010086. PMID: 33435214; PMCID: PMC7827407.
[4]. Jia S, Hu C. Pharmacological effects of rutaecarpine as a cardiovascular protective agent. Molecules. 2010 Mar 15;15(3):1873-81. doi: 10.3390/molecules15031873. PMID: 20336017; PMCID: PMC6257227.
[5]. Chan S, Sun R, Tu X, et al. Rutaecarpine suppresses the proliferation and metastasis of colon cancer cells by regulating the STAT3 signaling. J Cancer. 2022 Jan 1;13(3):847-857. doi: 10.7150/jca.66177. PMID: 35154453; PMCID: PMC8824880.
[6]. Wan J, Li M, Yuan X, et al. Rutaecarpine ameliorates osteoarthritis by inhibiting PI3K/AKT/NF?κB and MAPK signalling transduction through integrin αVβ3. Int J Mol Med. 2023 Oct;52(4):97. doi: 10.3892/ijmm.2023.5300. Epub 2023 Sep 1. PMID: 37654229; PMCID: PMC10555473.
[7]. Surbala L, Singh CB, Devi RV, et al. Rutaecarpine exhibits anti-diabetic potential in high fat diet-multiple low dose streptozotocin induced type 2 diabetic mice and in?vitro by modulating hepatic glucose homeostasis. J Pharmacol Sci. 2020 Aug;143(4):307-314. doi: 10.1016/j.jphs.2020.04.008. Epub 2020 Jun 9. PMID: 32536591.
[8]. Xu M, Shi Z, He Z, et al. Rutaecarpine alleviates migraine in nitroglycerin-induced mice by regulating PTEN/PGK1 signaling pathway to activate NRF2 antioxidant system. Biomed Pharmacother. 2023 Oct;166:115300. doi: 10.1016/j.biopha.2023.115300. Epub 2023 Aug 7. PMID: 37557014.
[9]. Jeon TW, Jin CH, Lee SK, et al. Immunosuppressive effects of rutaecarpine in female BALB/c mice. Toxicol Lett. 2006 Jul 1;164(2):155-66. doi: 10.1016/j.toxlet.2005.12.005. Epub 2006 Jan 18. PMID: 16412592.
| Experimentos celulares [1]: | |
Líneas celulares | Condrocitos de ratón |
Método de preparación | Los condrocitos de ratón se expusieron a IL?1β (5ng/ml) con Rutaecarpine (1, 2.5, 5 y 10µM) durante 24 horas, luego se determinaron los niveles de expresión de proteínas de MMP3, MMP13, IL?1β, COX2, IL?6, TNF?α, SOX9, COL II y agrecan se determinaron mediante análisis de transferencia occidental. |
Condiciones de reacción | 1, 2.5, 5 y 10µM, 24 horas |
Áreas de aplicación | Rutaecarpine atenúa la expresión inducida por IL?1β de citoquinas inflamatorias (COX2, IL?6, TNF?α e IL?1β) de una manera dependiente de la concentración en los condrocitos de ratón. |
| Experimentos con animales [2]: | |
Modelos animales | Ratón con migraña crónica |
Método de preparación | La migraña crónica (CM) fue tratada con Rutaecarpine (5, 10, 20mg/kg) y luego los marcadores asociados con el estrés oxidativo se examinaron mediante kits bioquímicos en el núcleo caudal del trigémino. |
Forma de dosificación | 5, 10, 20mg/kg/d, 9 días, i.g. |
Áreas de aplicación | El tratamiento con Rutaecarpine mejoró la migraña inducida por NTG en ratones al inhibir el estrés oxidativo. |
References: | |
| Cas No. | 84-26-4 | SDF | |
| Sinónimos | NSC 258317 | ||
| Chemical Name | 7,8-dihydroindolo[2',3':3,4]pyrido[2,1-b]quinazolin-5(13H)-one | ||
| Canonical SMILES | O=C1N(C2=NC3=C([H])C([H])=C([H])C([H])=C13)C([H])([H])C([H])([H])C4=C2N([H])C5=C([H])C([H])=C([H])C([H])=C45 | ||
| Formula | C18H13N3O | M.Wt | 287.32 |
| Solubility | DMF: 33 mg/ml,DMSO: 12 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4804 mL | 17.4022 mL | 34.8044 mL |
| 5 mM | 696.1 μL | 3.4804 mL | 6.9609 mL |
| 10 mM | 348 μL | 1.7402 mL | 3.4804 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)