research use only
Cat.No.S5676
| Related Targets | Adrenergic Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR |
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| Other Estrogen/progestogen Receptor Inhibitors | Elacestrant (RAD1901) Dihydrochloride Vepdegestrant (ARV-471) MPP dihydrochloride Kaempferol Cholesterol G15 Endoxifen HCl AZD9496 Chrysin Licochalcone A |
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In vitro |
DMSO
: 64 mg/mL
(201.03 mM)
Ethanol : 64 mg/mL Water : Insoluble |
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In vivo |
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| Molecular Weight | 318.36 | Formula | C18H22O5 |
Storage (From the date of receipt) | 3 years -20°C powder |
|---|---|---|---|---|---|
| CAS No. | 17924-92-4 | -- | Storage of Stock Solutions |
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| Synonyms | F2 toxin, RAL | Smiles | CC1CCCC(=O)CCCC=CC2=C(C(=CC(=C2)O)O)C(=O)O1 | ||
| Targets/IC50/Ki |
ERβ
165.7 nM
ERα
240.4 nM
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|---|---|
| In vitro |
Zearalenone is able to occupy the active site of ERs in a strikingly similar manner as E2. This compound disrupts genome stability and inhibits growth of porcine granulosa cells via the estrogen receptors which may promote granulosa cell apoptosis when the DNA repair system is not enough to rescue this serious damage. At low concentrations, it enhances cell proliferation, increases colony formation and fastens cell migration after wound healing. This chemical exhibits carcinogenesis-like properties.
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| In vivo |
In ovariectomized female ICR mice, s.c. administration of ZEN at doses ≥2 mg/kg/day for 3 consecutive days significantly increased uterine wet weight compared with the control group. This compound is an immunotoxic compound similar to estrogen and some endocrine disruptors. After oral exposure, ZEA is rapidly absorbed and initially metabolized by the intestinal tissue and hepatocytes; this initiates the biotransformation of the compound into its major biologically active reductive metabolites, α- and β-zearalenol (α- and β-ZOL). The estrogenic activity of this chemical and its metabolites is mediated by their binding affinity to estrogen receptors (ER), and they are as potent as coumestrol and genistein, two endocrine-disrupting phytestrogens.
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05751031 | Recruiting | HIV Infections |
Fondazione Penta UK|UCL Great Ormond Street Institute of Child Health|PENTA Foundation |
February 20 2023 | -- |
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