耗材描述
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。
产品来源： https://www.medchemexpress.cn/steppogenin.html
研究领域：Metabolic Enzyme/Protease
作用靶点：HIF/HIF Prolyl-Hydroxylase
来源：植物 | 桑科 | 柘
结构分类：黄酮类 | 黄酮 | 结构分类
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
相关产品：Deferoxamine mesylate | DMOG | PX-478 | Roxadustat | Minocycline hydrochloride | LW6 | Belzutifan | Chloramphenicol | PT-2385 | Chlorogenic acid | Daprodustat | BAY 87-2243 | Amifostine | Oltipraz | Molidustat | KC7F2 | Vadadustat | Glucosamine | IOX2 | E3330 | Oroxylin A | PT2399 | ML228 | Albendazole | IOX4 | AKBA | Cryptochlorogenic acid | Enarodustat | Bavachinin
品牌介绍: MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物；10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；设有专业的实验中心和严格的质控、验证体系；提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；产品的生物活性多经各国客户实验验证；Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；与世界各大制药公司及知名科研机构建立了长期的合作。
