Protodioscin, a major steroidal saponin in dioscoreae rhizome, has been shown to exhibit multiple biological actions, such as anti-hyperlipidemia, anti-cancer, sexual effects and cardiovascular properties. Protodioscin is able to stimulate testosterone production and it also has an androgen-mimetic action, binding and activating the testosterone receptors.
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产品名称 | Androgen Receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Cyproterone acetate |
++++
Androgen Receptor, IC50: 7.1 nM |
98% | |||||||||||||||||
Apalutamide |
+++
Androgen Receptor, IC50: 16 nM |
98% | |||||||||||||||||
AZD3514 |
+
Androgen Receptor, Ki: 2.2 μM |
98% | |||||||||||||||||
Darolutamide |
++++
Androgen receptor, Ki: 11 nM |
98% | |||||||||||||||||
Flutamide |
+++
Androgen Receptor, Ki: 55 nM |
98% | |||||||||||||||||
Galeterone |
++
Androgen Receptor, IC50: 384 nM |
98% | |||||||||||||||||
Enzalutamide |
+++
Androgen Receptor, IC50: 36 nM |
98% | |||||||||||||||||
Megestrol | ✔ | 98% | |||||||||||||||||
Bicalutamide |
++
Androgen Receptor, IC50: 0.16 μM |
99% | |||||||||||||||||
EPI-001 |
+
Androgen Receptor, IC50: ~6 μM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Protodioscin, a major steroidal saponin in dioscoreae rhizome, has been shown to exhibit multiple biological actions, such as anti-hyperlipidemia, anti-cancer, sexual effects and cardiovascular properties. Protodioscin (5 and 10 mg/kg) significantly improves glucose intolerance and reduced the levels of serum UA, BUN, Cr, TC (serum uric acid, blood urea nitrogen, creatinine, total cholesterol, triglyceride) and TG. Protodioscin significantly reduces renal concentrations of IL-1β, IL-6 and TNF-α by inhibiting the activation of nuclear factor-κB, c-Jun N-terminal kinase, p38 mitogen-activated protein kinase and extracellular signal-regulated kinase[3]. PD (Protodioscin) inhibits cell viability, causes a loss of mitochondrial function, and induces apoptosis, as evidenced by up-regulation of caspase-8, -3, -9, -PARP, and Bax activation, and down-regulation of Bcl-2 expression. PD was shown to induce ROS and the ER stress pathway, including GRP78, p-eIF-2α, ATF4, and CHOP[4]. Protodioscin ameliorates the death rate, inhibits the increase in neurological deficit scores and infarct volume, and reduces the apoptotic nerve cells induced by MCAO (middle cerebral artery occlusion) in rats. Protodioscin attenuates the change of relevant apoptins, suppresses the release of pro-inflammatory cytokines in serum and reverses the protein expression of NF-κB (in nucleus and cytoplasm) and IκBα (in cytoplasm) induced by MCAO in rats[5]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
0.95mL 0.19mL 0.10mL |
4.77mL 0.95mL 0.48mL |
9.53mL 1.91mL 0.95mL |
CAS号 | 55056-80-9 |
分子式 | C51H84O22 |
分子量 | 1049.199 |
别名 | NSC 698796 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,2-8°C |
溶解度 |
DMSO: 50 mg/mL(47.66 mM),配合低频超声助溶,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 H2O: 50 mg/mL(47.66 mM),配合低频超声助溶 |
动物实验配方 |