GR3027
产品编号: DC11090
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应用领域
GR3027(Golexanolone)是一种GABA-a受体调节类固醇拮抗剂,可选择性拮抗别孕烯醇酮和THDOC等神经甾体对GABAA受体的增强活化;抑制α1β2γ2L受体29±5%的THDOC增强GABA反应,不拮抗GABA对GABAA受体的作用;在用于不同受体的特定条件下,α1β2γ2LGABAA受体的IC50=250nM,α5β3γ2LGABAA受体的IC50=350nM;恢复慢性高氨血症和肝性脑病大鼠的空间学习和运动协调。睡眠障碍2期临床
Cas No.: |
2089238-18-4 |
名称: |
(17E)-3α-ethynyl-17-(hydroxyimino)-5α-androstan-3β-ol |
别名: |
GR-3027;Golexanolone |
SMILES: |
C[C@]12CC[C@](C[C@@H]1CC[C@@H]3[C@@H]2CC[C@]\4([C@H]3CC/C4=N\O)C)(C#C)O |
分子式: |
C21H31NO2 |
分子量: |
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纯度: |
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保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: |
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In Vivo: |
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In Vitro: |
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References: |
GR3027 (Golexanolone) is a GABA-A receptor modulating steroid antagonist that selectively antagonizes the enhanced activation of GABAA receptors by neurosteroids such as allopregnanolone and THDOC; inhibits α1β2γ2L receptor 29 ± 5% of THDOC enhancement of the GABA response, does not antagonize the effect of GABA at the GABAA receptor; during the specific conditions used for the different receptors, IC50=250 nM for the α1β2γ2L GABAA receptor and 350 nM for the α5β3γ2L GABAA receptor; restores spatial learning and motor coordination in rats with chronic hyperammonemia and hepatic encephalopathy. |
Kinase Assay: |
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Cell Assay: |
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Animal Administration: |
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References: |
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MSDS
COA
LOT NO. |
DOWNLOAD |
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2018-0101 |
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