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孕二烯二酮 /(Z)-Guggulsterone {[allProObj[0].p_purity_real_show]}

货号:A1144321 同义名: Z-Guggulsterone

(Z)-Guggulsterone is a broad spectrum steroid receptor ligand and an antagonist of FXR with antiseptic, antirheumatic and anti-inflammatory activity in vivo.

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
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Inaccessible (Haz class 6.1), International USD 150+
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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
(Z)-Guggulsterone 化学结构 CAS号:39025-23-5
(Z)-Guggulsterone 化学结构
CAS号:39025-23-5
(Z)-Guggulsterone 3D分子结构
CAS号:39025-23-5
(Z)-Guggulsterone 化学结构 CAS号:39025-23-5
(Z)-Guggulsterone 3D分子结构 CAS号:39025-23-5
规格 价格 会员价 库存 数量
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(Z)-Guggulsterone 纯度/质量文件 产品仅供科研

货号:A1144321 标准纯度: {[allProObj[0].p_purity_real_show]}
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(Z)-Guggulsterone 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].

(Z)-Guggulsterone 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.

(Z)-Guggulsterone 实验方案

计算器
存储液制备 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

(Z)-Guggulsterone 技术信息

CAS号39025-23-5
分子式C21H28O2
分子量 312.446
别名 Z-Guggulsterone
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

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

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