Steppogenin
Based on 1 Customer Validation
Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors.
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。
- 純度: 99.49%
- CAS 番号: 56486-94-3
- 分子式: C15H12O6
- 分子量:288.25
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
生物活性
IC50: 0.56 ± 0.043 μM (HIF-1α), 8.46 ± 1.08 μM (DLL4)[1]
Steppogenin (0-10 μM, 24 h) inhibit the transcriptional activity of HIF-1α under hypoxic conditions in HEK293T cells and VEGF-induced DLL4 expression in vascular endothelial cells (ECs) in a dose-dependent manner[1].
Steppogenin (0-3 μM, 6 h) suppresses the mRNA expression of HIF-1α target genes (VEGF, GLUT1, CXCR4, and CA9) under hypoxic conditions[1].
Steppogenin (0-3 μM, 16 h) suppresses HIF-1α protein levels, and inhibits protein levels of VEGF, CXCR4, and CA9[1].
Steppogenin (0-3 μM, 24 h) suppresses hypoxia-induced vascular EC proliferation and migration as well as VEGF-induced sprouting of EC spheroids[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:0, 0.3, 1, 3 μM
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Incubation Time:6 h
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Result:Suppressed the mRNA expression of HIF-1α target genes (VEGF, GLUT1, CXCR4, and CA9) under hypoxic conditions.
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Cell Line:HEK293T, A549, ARPE19 cells
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Concentration:0, 0.3, 1, 3 μM
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Incubation Time:16 h
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Result:Significantly suppressed HIF-1α protein levels in a dose-dependent manner. reduced nuclear expression of HIF-1α under hypoxic conditions. Inhibited protein levels of VEGF, CXCR4, and CA9 compared with the levels detected in the vehicle control group. Suppresseed VEGF-induced DLL4 protein expression.
Steppogenin (2 mg/kg, IP, once) shows the highest distribution to the liver and spleen (25.5-fold and 9.74-fold AUC ratio, respectively) with significantly higher T1/2[1].
Pharmacokinetic Parameters of Steppogenin in male C57BL/6 J mice[1].
| Cmax (ng/mL) | Tmax (h) | T1/2 (h) | AUC8h (ng/mL∗h) | AUC∞ (ng/mL∗h) | AUC ratio | |
| Plasma | 448 ± 113 | 0.25 | 0.49 ± 0.14 | 283 ± 98.9 | 284 ± 97.8 | 1 |
| Tumor | 635 ± 114 | 0.3 ± 0.1 | 1.87 ± 0.87 | 1078 ± 494 | 1252 ± 547 | 4.58 |
| Liver | 4319 ± 1063 | 0.25 | 1.72 ± 0.26 | 6733 ± 1300 | 6967 ± 1200 | 25.5 |
| Lung | 521 ± 181 | 0.25 | 0.36 ± 0.12 | 261 ± 96.1 | 280 ± 106 | 1.02 |
| Heart | 285 ± 15.2 | 0.25 | 0.2 | 107 ± 44.3 | 176.9 | 0.65 |
| Kidney | 1225 ± 463 | 0.25 | 0.33 ± 0.01 | 628 ± 234 | 624.7 ± 238 | 2.35 |
| Spleen | 6110 ± 2954 | 0.25 | 0.47 ± 0.01 | 2443 ± 1155 | 2663 ± 1289 | 9.74 |
| Brain | 309 ± 95.7 | 0.25 | 1.36 ± 0.46 | 191 ± 67 | 241 ± 75.4 | 0.88 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 J mice (6-week-old, male, Lewis lung carcinoma (LLC) allograft tumor model)[1]
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Dosage:2 mg/kg
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Administration:IP, once
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Result:Significantly suppressed tumor growth.
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Animal Model:C57BL/6 J mice (6-week-old, male, Lewis lung carcinoma (LLC) allograft tumor model)[1]
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Dosage:2 mg/kg
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Administration:IP, once (Pharmacokinetic Analysis)
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Result:Showed the highest distribution to the liver and spleen (25.5-fold and 9.74-fold AUC ratio, respectively) with significantly higher T1/2. may not be accumulated even in the highly distributed tissues after the repeated administration of steppogenin.
化学情報
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CAS 番号 56486-94-3
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性状 Solid
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分子量 288.25
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分子式 C15H12O6
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Color White to off-white
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SMILES
O=C1C[C@@H](C2=CC=C(O)C=C2O)OC3=CC(O)=CC(O)=C13
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Structure Classification
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Initial Source
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
DMSO : 3 mg/mL (10.41 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (279 KB)
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SDS (393 KB)
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- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4692 mL | 17.3461 mL | 34.6921 mL | 86.7303 mL |
| 5 mM | 0.6938 mL | 3.4692 mL | 6.9384 mL | 17.3461 mL | |
| 10 mM | 0.3469 mL | 1.7346 mL | 3.4692 mL | 8.6730 mL |