L-803,087 TRIFLUOROACETATE
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- CAS号:
- 217480-26-7
- 英文名:
- L-803,087 TRIFLUOROACETATE
- 英文别名:
- L803087,L 803087;L-803,087 TRIFLUOROACETATE;L-Arginine, N2-[4-(5,7-difluoro-2-phenyl-1H-indol-3-yl)-1-oxobutyl]-, methyl ester;N2-[4-(5,7-DIFLUORO-2-PHENYL-1H-INDOL-3-YL)-1-OXOBUTYL]-L-ARGININE METHYL ESTER TRIFLUOROACETATE
- 中文名:
- L-803,087 TRIFLUOROACETATE
- 中文别名:
- 化合物 T11800
- CBNumber:
- CB8840994
- 分子式:
- C25H29F2N5O3
- 分子量:
- 485.53
- MOL File:
- 217480-26-7.mol
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L-803,087 TRIFLUOROACETATE化学性质
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密度:
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1.33±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble to 100 mM in DMSO and to 100 mM in ethanol
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形态:
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Powder
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酸度系数(pKa):
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14.54±0.46(Predicted)
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L-803,087 TRIFLUOROACETATE性质、用途与生产工艺
L-803087 是一种有效的选择性的生长抑素 sst4 受体激动剂，Ki 为 0.7 nM，比其他生长抑素受体的选择性高 280 倍以上。L-803087 在体外促进 AMPA 介导的海马突触反应，在体内增加了海藻酸盐诱导的小鼠癫痫发作。
Ki: 0.7 nM (sst4 receptor), 199 nM (sst1 receptor), 4720 nM (sst2 receptor), 1280 nM (sst3 receptor) and 3880 nM (sst5 receptor)
L-803087 has
K
i
values for cloned human sst1, sst2, sst3 and sst5 receptors of 199, 4720, 1280 and 3880 nM, respectively.
L-803087 has a diamine moiety that maps to lysine on the phmacophore, but relation of this molecule to the aromatic and the Trp substituents of the phmacophore are not obvious. L-803087 does not inhibit secretion of growth hormone, insulin, or glucagon.
L-803087 (5 nmol) is doubled seizure activity in wild-type mice on average. Interestingly, this effect is blocked by 3 nmol Octreotide. In hippocampal slices from wild-type mice, Octreotide (2 μM) does not modify AMPA-mediated synaptic responses while facilitation occurred with L-803087 (2 μM).
L-803,087 TRIFLUOROACETATE
上下游产品信息
上游原料
下游产品
L-803,087 TRIFLUOROACETATE
生产厂家
217480-26-7, L-803,087 TRIFLUOROACETATE 相关搜索:
- Somatostatin receptor
- C25H29F2N5O3
- C25H29F2N5O3CF3CO2H
- 化合物 T11800
- 217480-26-7
- L803087,L 803087
- L-Arginine, N2-[4-(5,7-difluoro-2-phenyl-1H-indol-3-yl)-1-oxobutyl]-, methyl ester
- L-803,087 TRIFLUOROACETATE
- N2-[4-(5,7-DIFLUORO-2-PHENYL-1H-INDOL-3-YL)-1-OXOBUTYL]-L-ARGININE METHYL ESTER TRIFLUOROACETATE