HPTE
HPTE is the active in vivo metabolite of Methoxychlor (HY-B1873), and acts as an inhibitor of 3β‑HSD and 17β‑HSD3. HPTE binds to the substrate-binding pocket of 3β‑HSD in a non-competitive manner, but competitively occupies the coenzyme NAD+-binding site, thereby inhibiting the conversion of pregnenolone to progesterone. HPTE binds to the androstenedione-binding pocket (the substrate pocket) of 17β‑HSD3 in a non-competitive manner, and competitively occupies the coenzyme NADPH-binding site, thus blocking the conversion of androstenedione to testosterone. HPTE interferes with androgen biosynthesis in Leydig cells by inhibiting the activities of these two key steroidogenic enzymes. HPTE can be used in studies related to androgen biosynthesis.
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- No. CAS: 2971-36-0
- Fòrmula: C14H11Cl3O2
- Peso molecular:317.59
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Ver todos los productos específicos de isoformas 17β-HSD
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
17β-HSD5 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | EC50 |
30.7 nM
Compound: BPE-Cl; HPTE
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Agonist activity at ERalpha (unknown origin) expressed in human HeLa cells assessed as transcriptional activation measured after 24 hrs by luciferase reporter gene assay
Agonist activity at ERalpha (unknown origin) expressed in human HeLa cells assessed as transcriptional activation measured after 24 hrs by luciferase reporter gene assay
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[PMID: 31879182] |
| HeLa | IC50 |
85.4 nM
Compound: BPE-Cl; HPTE
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Antagonist activity at ERbeta (unknown origin) expressed in human HeLa cells assessed as inhibition of E2-induced transcriptional activity measured after 24 hrs by luciferase reporter gene assay based Schild plot analysis
Antagonist activity at ERbeta (unknown origin) expressed in human HeLa cells assessed as inhibition of E2-induced transcriptional activity measured after 24 hrs by luciferase reporter gene assay based Schild plot analysis
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[PMID: 31879182] |
In Vitro
HPTE inhibits the activity of human testicular microsomal 3β-HSD with an IC50 of 8.29 μM, and inhibits the activity of rat testicular microsomal 3β-HSD with an IC50 of 13.82 μM. It acts as a non-competitive inhibitor of the substrate PREG and a competitive inhibitor of the cofactor NAD+[1].
HPTE inhibits the activity of human testicular microsomal 17β-HSD3 with an IC50 of 12.12 μM, and inhibits the activity of rat testicular microsomal 17β-HSD3 with an IC50 of 32.0 μM. It acts as a non-competitive inhibitor of the substrate DIONE and a competitive inhibitor of the cofactor NADPH[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2971-36-0
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Appearance Solid
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Peso molecular 317.59
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Fòrmula C14H11Cl3O2
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SMILES
ClC(Cl)(C(C1=CC=C(C=C1)O)C2=CC=C(C=C2)O)Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HPTE Related Classifications
HY-W490804 Related Classifications
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