Rutaevin
Based on 1 Customer Validation
Rutaevin is an antifungal toxin and CYP3A4 inactivator. Rutaevin requires NADPH-dependent bioactivation to generate cis-but-2-ene-1,4-dial, which then covalently modifies and mechanism-based inactivates human CYP3A4 (IC50=4.48 μM, Ki=15.98 μM), and interacts with substances such as glutathione. Rutaevin disrupts the cellular structure of Sirococcus conigenus, accumulates linearly in resistant larch after pathogen exposure, and induces liver toxicity in mice via oral administration. Rutaevin can be applied to research in fields related to larch shoot blight and other associated areas.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.77%
- CAS 番号: 33237-37-5
- 分子式: C26H30O9
- 分子量:486.51
-
保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
CYP3A4 4.48 μM (IC50) |
体外実験
Rutaevin (20-100 μM; 1-2 h) undergoes NADPH-dependent bioactivation to form a reactive BDA intermediate in rat and human liver microsomes, which reacts with nucleophilic trapping agents GSH, NAL, and MOA to form 10 distinct conjugates, including the cyclic mono(GSH) conjugate M1[1].
Rutaevin (0.1-30 μM; 30 min) acts as a potential mechanism-based inactivator of CYP3A4 in human liver microsomes, as shown by the 5.03-fold decrease in IC50 (to 4.48 μM) following NADPH-dependent preincubation[1].
Rutaevin (0.0625-1.0000 mg/mL; up to 5 days) potently inhibits the growth of Neofusicoccum laricinum with an IC50 of 0.27 mg/mL and achieves complete inhibition at 0.5 mg/mL[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
Rutaevin (oral) induces hepatotoxicity in mice, as indicated by elevated serum ALT and AST activities[1].
Rutaevin (p.o.) induces hepatotoxicity in mice via bioactivation processes[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Sprague-Dawley (male, 220-250 g, bile duct cannulated)[1]
-
Dosage:5 mg/kg
-
Administration:i.v.; single dose
-
Result:Detected a cyclic mono(GSH) conjugate of rutaevin's bioactivated cis-butene-1,4-dial (BDA) intermediate (designated M1) as the most abundant metabolite in rat bile samples.
化学情報
-
CAS 番号 33237-37-5
-
性状 Solid
-
分子量 486.51
-
分子式 C26H30O9
-
Color White to off-white
-
SMILES
C[C@]1([C@H]2O)[C@@]3([C@@H]4O3)[C@]([C@H](C5=COC=C5)OC4=O)(CC[C@]1([H])[C@]67[C@](C(C)(C)O[C@@]6([H])CC(OC7)=O)([H])C2=O)C
-
Structure Classification
-
Initial Source
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
プロトコル
-
How to Select the Route of Administration for Mammals
Route-of-administration selection in mammals is a pharmacokinetic, pharmacodynamic, formulation, animal-welfare, and translational decision, not a default technical choice. The selected route should match the study goal: intravenous dosing is most useful when complete systemic exposure and rapid onset are required, oral dosing is most translational for orally intended medicines but is affected by absorption and first-pass metabolism, subcutaneous or intramuscular dosing can provide slower systemic exposure, and intraperitoneal dosing can be useful in rodent proof-of-concept studies but may have limited clinical translation. Published route-comparison studies show that the same compound can produce different exposure, onset, bioavailability, tissue distribution, and tolerability depending on route; therefore, route choice should be supported by pilot pharmacokinetic or pharmacodynamic evidence when the literature is insufficient. Unresolved questions include how to standardize route sel
-
Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Hepatotoxicity Study
This protocol evaluates hepatotoxicity using complementary in vivo mouse APAP acute liver injury and in vitro hepatocyte-based cytotoxicity readouts. In vivo APAP injury is assessed by serum ALT/AST, liver histology, hepatic glutathione, protein adducts, necrosis, inflammation, and regeneration-related endpoints. In vitro hepatotoxicity is assessed by loss of viability, leakage of ALT/AST/LDH, oxidative-stress markers, mitochondrial function, nuclear morphology, intracellular calcium, and high-content imaging endpoints.
純度とドキュメンテーション
-
データシート (280 KB)
-
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)
-
取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Rutaevin 関連分類
HY-N2620 関連分類
Powered by Bioz