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(Z)-Guggulsterone

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Chemical Structure| 39025-23-5 同义名 : Z-Guggulsterone
CAS号 : 39025-23-5
货号 : A1144321
分子式 : C21H28O2
纯度 : 98+%
分子量 : 312.446
MDL号 : MFCD01310757
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 9 mg/mL(28.8 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Vascular Endothelial Growth Factors (VEGFs) and their receptors (VEGF-Rs) are important regulators for angiogenesis and lymphangiogenesis. VEGFs and VEGF-Rs are not only expressed on endothelial cells but also on various subtypes of solid tumors and leukemias contributing to the growth of the malignant cells[2]. VEGF rapidly induced tyrosine phosphorylation of type 1 and type 2 VEGF receptors. Physical association between VEGF-receptor 2 (VEGF-R2) and insulin receptor substrate (IRS-1) and phosphatidylinositol 3'-kinase (PI3K) was induced by VEGF, which augmented PI3K activity in VEGF-R2 immunoprecipitates[3]. In a human melanoma xenograft mouse model, blockade of both VEGF-R2 and Tie-2 pathways or the VEGF receptor pathway alone resulted in a significant inhibition of tumor growth and tumor angiogenesis (92.2 % and 74.4 %)[4]. (Z)-Guggulsterone inhibits the growth of human prostate cancer cells by causing apoptosis. Z-guggulsterone inhibits angiogenesis by suppressing the vascular endothelial growth factor (VEGF)-VEGF-R2–Akt signaling axis. In HUVEC, Z-guggulsterone (10, 20 μM; 24 or 48 hours) induces a reduction in the level of VEGF-R2 protein. In tumor volume and wet tumor weight, Z-guggulsterone (p.o.; 1 mg; 5 times/week) causes a statistically significant reduction[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.20mL

0.64mL

0.32mL

16.00mL

3.20mL

1.60mL

32.01mL

6.40mL

3.20mL
参考文献

[1]Meyer U, Costantino G, Macchiarulo A, Pellicciari R. Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. J Med Chem. 2005 Nov 3;48(22):6948-55. doi: 10.1021/jm0505056. PMID: 16250653.

[2]Hilmar Quentmeier, DNA methylation regulates expression of VEGF-R2 (KDR) and VEGF-R3 (FLT4). BMC Cancer. 2012 Jan 17;12:19.

[3]Denis Feliers,et al. VEGF regulation of endothelial nitric oxide synthase in glomerular endothelial cells. Kidney Int. 2005 Oct;68(4):1648-59.

[4]N Jendreyko,et al. Simultaneous, phenotypic knockout of VEGF-R2 and Tie-2 with an intradiabody enhances antiangiogenic effects in vivo.Klin Padiatr. May-Jun 2006;218(3):143-51.

[5]Xiao D, et al. z-Guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, inhibits angiogenesis in vitro and in vivo. Mol Cancer Ther. 2008 Jan;7(1):171-80.