Escholtzine
Escholtzine is an Alkaloid. Escholtzine can be isolated from Eschscholzia californica. Escholtzine is a CYP3A4 inhibitor, 5-HT1A receptor inhibitor with a CYP3A4 IC50 of 13.4 μM, 5-HT1A EC50 of 11 μM. Escholtzine can be used for the research of anxiety, depression.
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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: 4040-75-9
- 分子式: C19H17NO4
- 分子量:323.34
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保管条件:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
5-HT Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
5-HT1A Receptor 11 μM (EC50) |
CYP3A4 13.4 μg/mL (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
8.709 μM
Compound: 3
|
Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
|
[PMID: 28099003] |
| CHO | EC50 |
11 μM
Compound: 2
|
Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells
Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells
|
[PMID: 16562853] |
| KB | IC50 |
17.03 μM
Compound: 3
|
Antiproliferative activity against human KB cells after 72 hrs by SRB assay
Antiproliferative activity against human KB cells after 72 hrs by SRB assay
|
[PMID: 28099003] |
| MCF7 | IC50 |
26.56 μM
Compound: 3
|
Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay
Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay
|
[PMID: 28099003] |
| MDA-MB-231 | IC50 |
26.13 μM
Compound: 3
|
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
|
[PMID: 28099003] |
体外実験
Escholtzine (60 min) weakly inhibits the binding of [3H]8-OH-DPAT to human recombinant 5-HT1A receptors, with an EC50 of 11 μM and a Ki of 6 μM[1].
Escholtzine (1 h) potently inhibits CYP3A4 enzyme activity in vitro, with an IC50 value of 13.4 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
化学情報
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CAS 番号 4040-75-9
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性状 Solid
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分子量 323.34
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分子式 C19H17NO4
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Color White to off-white
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SMILES
[H][C@]1(N2C)CC3=CC4=C(OCO4)C=C3[C@]2([H])CC5=CC6=C(OCO6)C=C51
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Structure Classification
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Initial Source
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
プロトコル
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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.
純度とドキュメンテーション
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データシート (271 KB)
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SDS (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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取扱説明書 (2659 KB)
参考文献
[1]. Gafner S, et al. Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro. J Nat Prod. 2006 Mar;69(3):432-5. [Content Brief]
[2]. Cahlíková L, et al. Acetylcholinesterase and butyrylcholinesterase inhibitory compounds from Eschscholzia californica (Papaveraceae). Nat Prod Commun. 2010;5(7):1035-1038. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)