1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. Steppogenin

Steppogenin  (Synonyms: 草大戟素)

目录号: HY-122094
产品使用指南

Steppogenin 是一种有效的 HIF-1αDLL4 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。

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Steppogenin Chemical Structure

Steppogenin Chemical Structure

CAS No. : 56486-94-3

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查看 HIF/HIF Prolyl-Hydroxylase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

IC50 & Target

IC50: 0.56 ± 0.043 μM (HIF-1α), 8.46 ± 1.08 μM (DLL4)[1]

体外研究
(In Vitro)

Steppogenin (0-10 μM, 24 h) 以剂量依赖性方式抑制 HEK293T 细胞缺氧条件下 HIF-1α 的转录活性和血管内皮细胞 (ECs) 中 VEGF 诱导的 DLL4 表达[1]
Steppogenin (0-3 μM,6 h) 在缺氧条件下抑制 HIF-1α 靶基因(VEGF、GLUT1、CXCR4 和 CA9)的 mRNA 表达[1]
Steppogenin (0-3 μM,16 h) 抑制 HIF-1α 蛋白水平,并抑制 VEGF、CXCR4 和 CA9 的蛋白水平[1]
Steppogenin (0-3 μM,24 h) 抑制缺氧诱导的血管 EC 增殖和迁移以及 VEGF 诱导的 EC 球体发芽[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR[1]

Cell Line: A549 cells
Concentration: 0, 0.3, 1, 3 μM
Incubation Time: 6 h
Result: Suppressed the mRNA expression of HIF-1α target genes (VEGF, GLUT1, CXCR4, and CA9) under hypoxic conditions.

Western Blot Analysis[1]

Cell Line: HEK293T, A549, ARPE19 cells
Concentration: 0, 0.3, 1, 3 μM
Incubation Time: 16 h
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.
体内研究
(In Vivo)

Steppogenin (2 mg/kg,腹腔注射,一次) 抑制肿瘤生长和血管生成[1]
Steppogenin (2 mg/kg,腹腔注射,一次) 在肝脏和脾脏中的分布最高 (分别为 25.5 倍和 9.74 倍 AUC 比率),T1/2 显著更高[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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 J mice (6-week-old, male, Lewis lung carcinoma (LLC) allograft tumor model)[1]
Dosage: 2 mg/kg
Administration: IP, once
Result: Significantly suppressed tumor growth.
Animal Model: C57BL/6 J mice (6-week-old, male, Lewis lung carcinoma (LLC) allograft tumor model)[1]
Dosage: 2 mg/kg
Administration: IP, once (Pharmacokinetic Analysis)
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.
分子量

288.25

Formula

C15H12O6

CAS 号
中文名称

草大戟素

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Steppogenin
目录号:
HY-122094
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