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| 产品名称 | GABA receptor ↓ ↑ | GABAA receptor ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Niflumic Acid | ✔ | 98% | |||||||||||||||||
| Ginkgolide A |
++
GABA receptor, Ki: 14.5 μM |
98% | |||||||||||||||||
| Valproic acid sodium | ✔ | HDAC,Autophagy | 97% | ||||||||||||||||
| Flumazenil | ✔ | 95% | |||||||||||||||||
| Bemegride | ✔ | 98% | |||||||||||||||||
| Bicuculline |
+++
GABAA receptor, IC50: 2 μM |
99% | |||||||||||||||||
| 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。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | Ginkgolide A is a highly active platelet activating factor antagonist cage molecule which was isolated from the leaves of the Ginkgo biloba L. Ginkgolide A may be one of the potential therapeutic lead compounds, especially for the treatment of cardiovascular, hepatological, and neurological diseases and disorders[3]. Ginkgolide-A (GA), a natural PXR ligand, attenuated BT in cirrhotic mice by abrogating inflammation along the gut-liver-axis, and by protecting small intestinal tight junctions (TJ)[4]. GA could suppress the expression of pro-inflammatory mediators (cyclooxygenase-2 (COX-2) and nitric oxide (NO) and pro-inflammatory cytokines (tumor necrosis factor (TNF)-α, interleukin (IL)-6 and IL-1β) in LPS-treated mouse peritoneal macrophages, mouse macrophage RAW264.7 cells, and differentiated human monocytes (dTHP-1) in vitro[5]. GA is non-toxic at high concentrations in hepatocytes. Moreover, GA was found to inhibit cellular lipogenesis and lipid accumulation by causing mitochondrial oxidative stress. GA showed hepatoprotective efficacy by inducing cellular lipoapoptosis and by inhibiting cellular inflammation[6]. |
| Concentration | Treated Time | Description | References | |
| Rat pulmonary microvascular endothelial cells (PMVECs) | 5-10 μg/mL | 22 hours | Inhibition of PMVEC apoptosis, significantly increased c-Myc mRNA expression and suppressed Bcl-2 mRNA reduction at 5-10 μg/mL concentration. | Biosensors (Basel). 2021 Aug 6;11(8):264 |
| human aortic smooth muscle cells (HASMC) | 50 μM GA | 24 hours | To investigate the effect of GA on GABRA3 expression in HASMCs, results showed significant reduction in GABRA3 protein expression after GA treatment | Redox Biol. 2024 Nov;77:103397 |
| differentiated THP-1 cells | 0-20 μg/mL | 24 hours | Inhibited LPS-induced COX-2 expression, downregulated pro-inflammatory cytokines TNF-α, IL-6, and IL-1β | Int J Mol Sci. 2017 Apr 10;18(4):794 |
| RAW264.7 cells | 0-20 μg/mL | 24 hours | Inhibited LPS-induced COX-2 expression and NO production, downregulated pro-inflammatory cytokines TNF-α, IL-6, and IL-1β | Int J Mol Sci. 2017 Apr 10;18(4):794 |
| mouse peritoneal macrophages | 0-20 μg/mL | 24 hours | Inhibited LPS-induced COX-2 expression and NO production, downregulated pro-inflammatory cytokines TNF-α, IL-6, and IL-1β | Int J Mol Sci. 2017 Apr 10;18(4):794 |
| Wharton's Jelly-derived mesenchymal stem cells (WJMSCs) | 80 µM | 5 days | To evaluate the effect of GA on WJMSCs proliferation, results showed that GA promoted WJMSCs proliferation. | Aging (Albany NY). 2023 Feb 20;15(5):1358-1370 |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | AngII-induced AAA model and Ca3(PO4)2-induced AAA model | Intragastric administration | 100 mg/kg body weight | Once daily for 28 days | To investigate the protective effect of GA on AAA formation, results showed GA treatment significantly suppressed AAA formation and progression | Redox Biol. 2024 Nov;77:103397 |
| BALB/c mice | LPS-induced inflammation model | Intraperitoneal injection | 20 mg/kg | Single dose, samples collected after 2 hours | Inhibited LPS-induced TNF-α and IL-6 production, activated AMPK signaling pathway | Int J Mol Sci. 2017 Apr 10;18(4):794 |
| C57BL6/J mice | Traumatic brain injury (TBI) model | Intraperitoneal injection | 5 mg/kg | Once daily for 7 days | Ginkgolide A improved neurological deficits in TBI mice by reducing oxidative stress and inhibiting apoptosis | Heliyon. 2024 Jan 14;10(2):e24759 |
| C57BL/6 mice | DCF1-knockout mice | Intraperitoneal injection | 10 mg/kg body weight | For 5 consecutive days | Inhibition of GABA partially rescued the visual deficit in DCF1-KO mice | Neurosci Bull. 2018 Jun;34(3):465-475 |
| C57BL/6 mice | CCl4-induced hepatitis and colitis model | Oral gavage | 50-200 mg/kg/day | Once daily for 3 days | Ginkgolide A significantly alleviated CCl4-induced hepatitis and colitis, reduced serum ALT and AST levels in a dose-dependent manner. | Biomol Ther (Seoul). 2016 Jan;24(1):40-8 |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT03772847 | Intravenous Alteplase Thrombol... 展开 >>ysis Neurological Improving 收起 << | Phase 4 | Recruiting | December 1, 2019 | China, Zhejiang ... 展开 >> Min Lou Recruiting Hangzhou, Zhejiang, China, 310000 Contact: Zexin Chen 13757118366 HREC2013@126.com 收起 << |
| NCT02425436 | Intrauterine Growth Restrictio... 展开 >>n (IUGR) 收起 << | Phase 2 | Completed | - | - |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.45mL 0.49mL 0.24mL |
12.24mL 2.45mL 1.22mL |
24.49mL 4.90mL 2.45mL |
|
| CAS号 | 15291-75-5 |
| 分子式 | C20H24O9 |
| 分子量 | 408.4 |
| SMILES Code | O[C@@]1([C@@H]2C)C34[C@]5(C([C@H]6O)([C@H](C(C)(C)C)C[C@@]5([H])OC4=O)[C@](OC6=O)([H])O3)C[C@]1([H])OC2=O |
| MDL No. | MFCD07437829 |
| 别名 | BN-52020 |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 105 mg/mL(257.1 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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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