Anizatrectinib
Anizatrectinib (hTrkA-IN-1) is an orally active and blood-brain barrier-penetrant TrkA kinase/hERG channel inhibitor. Anizatrectinib can be used for research on TrkA-mediated related diseases, such as pain, cancer, inflammation, and inflammatory diseases.
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。
- CAS 番号: 1824664-89-2
- 分子式: C29H32FN7O2
- 分子量:529.61
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
TrkA |
体外実験
Anizatrectinib (Compound 1) has decreased inhibitory activity against the hERG channel (IC50 = 20 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | AUC | Cmax |
|---|---|---|---|---|
| Rat[1] | 10 mg/kg mg/kg | p.o. | 2.57 μg·h/mL | 1.06 μg/mL |
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1824664-89-2
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分子量 529.61
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分子式 C29H32FN7O2
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SMILES
O=C(NC1=C(C)C(C2=CN=C(C)N=C2)=NN1C3=CC=CC=C3)N[C@@H]4CN(CCOC)C[C@H]4C5=CC=CC(F)=C5
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別名
hTrkA-IN-1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)