YM580
YM580 is a potent, orally active and selective Androgen Receptor (AR) antagonist (IC50 = 0.11 μM, hAR Ki = 4.6 nM, rAR Ki = 6.2 nM). YM580 exhibits good selectivity over PR, GR, and ERα (Kis > 3300 nM). YM580 decreases ventral prostate weight in mature intact rats dose-dependently without affecting serum testosterone levels. YM580 can be used for the research of prostate cancer.
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: 262295-11-4
- 分子式: C21H19F6N5O
- 分子量:471.41
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
Androgen Receptor|
hAR 4.6 nM (Ki) |
rAR 6.2 nM (Ki) |
rat PR 3300 nM (Ki) |
human GR >100000 nM (Ki) |
human ERα >100000 nM (Ki) |
体外実験
YM580 potently inhibits AR-mediated transcriptional activation in AR/CHO#3 cells, with an IC50 of 0.11 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Mature intact male Wistar rats (10-week-old)[1]
-
Dosage:0.3, 1, 3, 10, 30 mg/kg
-
Administration:p.o.; daily; 15 days
-
Result:Decreased ventral prostate weight in a dose-dependent manner with an ED50 of 2.2 mg/kg/day, and an inhibition rate of 67% at 10 mg/kg/day.
Exerted a maximum antiandrogenic effect comparable to surgical castration at 30 mg/kg/day.
Did not significantly elevate serum testosterone levels across all doses.
Exhibited good peripheral selectivity.
化学情報
-
CAS 番号 262295-11-4
-
分子量 471.41
-
分子式 C21H19F6N5O
-
SMILES
C[C@@H]1N(C2=CC(C(F)(F)F)=C(C#N)C=C2)C[C@@H](C)N(C(NC=3C=CC(C(F)(F)F)=NC3)=O)C1
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
-
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.
-
Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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)