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.
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: 2971-36-0
- 分子式: C14H11Cl3O2
- 分子量:317.59
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
17β-HSD 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]|
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
|
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
|
[PMID: 31879182] |
| HeLa | IC50 |
85.4 nM
Compound: BPE-Cl; HPTE
|
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
|
[PMID: 31879182] |
体外実験
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.
化学情報
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CAS 番号 2971-36-0
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性状 Solid
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分子量 317.59
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
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)