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.
For research use only. We do not sell to patients.
- CAS No.: 4040-75-9
- Formula: C19H17NO4
- Molecular Weight:323.34
-
Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
All 5-HT Receptor Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
5-HT1A Receptor 11 μM (EC50) |
CYP3A4 13.4 μg/mL (IC50) |
Cellular Effect
|
Cell Line
|
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] |
In Vitro
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.
Chemical Information
-
CAS No. 4040-75-9
-
Appearance Solid
-
Molecular Weight 323.34
-
Formula C19H17NO4
-
Color White to off-white
-
SMILES
[H][C@]1(N2C)CC3=CC4=C(OCO4)C=C3[C@]2([H])CC5=CC6=C(OCO6)C=C51
-
Structure Classification
-
Initial Source
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Protocols
-
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.
Purity & Documentation
-
Data Sheet (271 KB)
-
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)
-
Handling Instructions (2659 KB)
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)