SR210831C
SR210831C is a highly selective, orally active retinoic acid receptor α (RARα) inhibitor with an IC50 of 0.051 nM. SR210831C suppresses spermatogenesis by reducing sperm count in house mice via acting on the early stages of spermatogenesis, and it does not cross the blood-testis barrier. SR210831C can be used in male contraception research.
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。
- 分子式: C29H25NO3
- 分子量:435.51
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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RXR α 0.051 nM (IC50) |
SR210831C potently and selectively inhibits human RARα with an IC50 of 0.051 nM, showing >1647-fold selectivity over RARβ and >1960-fold selectivity over RARγ in GeneBLAzer reporter cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 (Plasma) | Cmax |
|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 12.0 h | 4992 ng/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD1 mice[1]
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Dosage:10 mg/kg/day; 1 mg/kg/day; 0.3 mg/kg/day; 0.1 mg/kg/day; 0.03 mg/kg/day
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Administration:p.o.; daily; 28 days
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Result:Reduced sperm counts to 2.6 × 106 per sample and testicular weight to 205 mg at 10 mg/kg/day.
Achieved complete inhibition of spermatogenesis 1 day post-treatment at 1 mg/kg/day and 0.3 mg/kg/day.
Showed reduced inhibitory effect on spermatogenesis 1 day post-treatment at 0.1 mg/kg/day.
Detected no inhibitory effect on spermatogenesis 1 day post-treatment at 0.03 mg/kg/day.
Recovered sperm counts to ~40% of control levels at 4 weeks post-treatment and fully recovered by 8 weeks post-treatment at 10 mg/kg/day.
Showed partial sperm count recovery at 4 weeks post-treatment and full recovery by 8 weeks post-treatment, with testicular weight returning to baseline by 4 weeks post-treatment at 1 mg/kg/day.
化学情報
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分子量 435.51
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分子式 C29H25NO3
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SMILES
CC1=C2O[C@H](C(C3=CC=C(N3)C4=CC=C(C=C4)C(O)=O)=CC2=C(C=C1)C5=CC=C(C)C=C5)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
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)