5'-Methoxynobiletin
Based on 1 Customer Validation
5'-Methoxynobiletin is a potent and orally active antinociceptive and anti-inflammatory agent. 5'-Methoxynobiletin is a polymethoxyflavone, that can be isolated from A. conyzoides.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.73%
- CAS. Nr.: 6965-36-2
- Formel: C22H24O9
- Molecular Weight:432.42
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| KB | ED50 |
0.5 μg/mL
Compound: NSC-67580
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Cytotoxicity against human KB cells
Cytotoxicity against human KB cells
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[PMID: 469554] |
In Vivo
5'-Methoxynobiletin (100 mg/kg, Orally, once) shows anti-nociceptive and anti-inflammatory activity[2].
5'-Methoxynobiletin (10 mg/kg (IV), 50 mg/kg (oral), once) showed a low oral bioavailability in rats, around 8-11%[2].
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MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss mice (female)[2]
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Dosage:100 mg/kg
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Administration:Orally
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Result:Significantly reduced both phases of formalin-induced nocifensive behavior after 15, 30 and 60 min of oral administration, when compared to control groups. In the neurogenic phase, inhibitions of 43±3%, 68±6% and 53±5% of the nociceptive response were observed, while for the infammatory phase inhibitions were 70±8%, 91±3% and 85±3% after 15, 30 and 60 min of the oral administration of 5'-Methoxynobiletin, respectively.
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Animal Model:Wistar rats (male)[2]
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Dosage:10 mg/kg (IV), 50 mg/kg (oral)
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Administration:IV, oral, once (Pharmacokinetic Analysis)
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Result:Pharmacokinetic Parameters of 5'-Methoxynobiletin in male Wistar rats[1].
IV (10 mg/kg) IG (50 mg/kg) λ (h-1) 0.55±0.03 0.29±0.2 Tmax (h) 2.71±0.49 Cmax (mg/L) 0.62±0.21 AUC0-∞ (mg·h/L) 8.19±4.1 3.65±0.8 t1/2 elimination (h) 1.26±0.1 2.31±0.9 CL (L/h.kg) 1.22±0.26 13.68±0.29 Vd, ss (L/kg) 2.24±0.32 47.46±10.10 F (%) 8.67
Chemical Information
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CAS. Nr. 6965-36-2
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Appearance Solid
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Molecular Weight 432.42
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Formel C22H24O9
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Color White to light yellow
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SMILES
O=C1C=C(C2=CC(OC)=C(OC)C(OC)=C2)OC3=C(OC)C(OC)=C(OC)C(OC)=C13
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Structure Classification
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 62.5 mg/mL (144.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Faqueti LG, et al. Antinociceptive and anti-inflammatory activities of standardized extract of polymethoxyflavones from Ageratum conyzoides. J Ethnopharmacol. 2016 Dec 24;194:369-377. [Content Brief]
[2]. Faqueti LG, et al. Preclinical Pharmacokinetic and Pharmacodynamic Investigation of 5'-Methoxynobiletin from Ageratum conyzoides: In vivo and In silico Approaches. Pharm Res. 2022 Sep;39(9):2135-2145. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.3126 mL | 11.5628 mL | 23.1257 mL | 57.8142 mL |
| 5 mM | 0.4625 mL | 2.3126 mL | 4.6251 mL | 11.5628 mL | |
| 10 mM | 0.2313 mL | 1.1563 mL | 2.3126 mL | 5.7814 mL | |
| 15 mM | 0.1542 mL | 0.7709 mL | 1.5417 mL | 3.8543 mL | |
| 20 mM | 0.1156 mL | 0.5781 mL | 1.1563 mL | 2.8907 mL | |
| 25 mM | 0.0925 mL | 0.4625 mL | 0.9250 mL | 2.3126 mL | |
| 30 mM | 0.0771 mL | 0.3854 mL | 0.7709 mL | 1.9271 mL | |
| 40 mM | 0.0578 mL | 0.2891 mL | 0.5781 mL | 1.4454 mL | |
| 50 mM | 0.0463 mL | 0.2313 mL | 0.4625 mL | 1.1563 mL | |
| 60 mM | 0.0385 mL | 0.1927 mL | 0.3854 mL | 0.9636 mL | |
| 80 mM | 0.0289 mL | 0.1445 mL | 0.2891 mL | 0.7227 mL | |
| 100 mM | 0.0231 mL | 0.1156 mL | 0.2313 mL | 0.5781 mL |
5'-Methoxynobiletin Related Classifications
HY-134602 Related Classifications
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