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CAS No. : 56486-94-3
MCE 国际站:Steppogenin
产品活性:Steppogenin 是一种有效的 HIF-1α 和 DLL4 的抑制剂,其 IC50 值分别为 0.56 和 8.46 μM。Steppogenin 可用于血管生成疾病的研究,如实体瘤。
研究领域:Metabolic Enzyme/Protease
作用靶点:HIF/HIF Prolyl-Hydroxylase
In Vitro: 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.
Steppogenin (0-3 μM, 6 h) suppresses the mRNA expression of HIF-1α target genes (VEGF, GLUT1, CXCR4, and CA9) under hypoxic conditions.
Steppogenin (0-3 μM, 16 h) suppresses HIF-1α protein levels, and inhibits protein levels of VEGF, CXCR4, and CA9.
Steppogenin (0-3 μM, 24 h) suppresses hypoxia-induced vascular EC proliferation and migration as well as VEGF-induced sprouting of EC spheroids.
In Vivo: Steppogenin (2 mg/kg, IP, once) inhibits tumor growth and angiogenesis.
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.
Pharmacokinetic Parameters of Steppogenin in male C57BL/6 J mice.
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 |
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