154106-92-0
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- CAS号:
- 154106-92-0
- 英文名:
- RPR 104632
- 英文别名:
- RPR 104632;RPR104632,RPR-104632;2H-1,2,4-Benzothiadiazine-3-carboxylic acid, 2-[(3-bromophenyl)methyl]-6,8-dichloro-3,4-dihydro-, 1,1-dioxide
- 中文名:
- 154106-92-0
- 中文别名:
- 化合物 T16797
- CBNumber:
- CB51368748
- 分子式:
- C15H11BrCl2N2O4S
- 分子量:
- 466.13
- MOL File:
- 154106-92-0.mol
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154106-92-0化学性质
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沸点:
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658.6±65.0 °C(Predicted)
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密度:
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1.788±0.06 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 in DMSO
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酸度系数(pKa):
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2.00±0.20(Predicted)
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154106-92-0性质、用途与生产工艺
RPR104632 是一种特异性的 NMDA receptor 拮抗剂,具有神经保护的作用。
RPR104632 antagonizes the binding of [
3
H]5,7-dichlorokynurenic acid to the rat cerebral cortex, with a K
i
of 4.9 nM. RPR104632 inhibits [
3
H]N-[1-(2-thienyl)cyclohexyl]-3,4-piperidine ([
3
H]TCP) binding in the presence of N-methyl-D-aspartate (NMDA) (IC
50
= 55 nM). RPR104632 inhibits the NMDA-evoked increase in guanosine 3',5'-cyclic monophosphate (cGMP) levels of neonatal rat cerebellar slices (IC
50
= 890 nM) in a non-competitive manner and markedly reduces NMDA-induced neurotoxicity in rat hippocampal slices and in cortical primary cell cultures. MK-801 (1 μM) completely protects the CA1 and CA3 pyramidal neurones against NMDA-induced toxicity, but these effects are not blocked by glycine. RPR104632 produces a significant and consistent neuroprotective effect towards all the NMDA-induced toxicity and has no effect when it is added alone at concentrations up to 10 μM. RPR104632 has neuroprotective potencies, with EC
50
of 4 μM.
154106-92-0
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上游原料
下游产品
154106-92-0, 154106-92-0 相关搜索:
- C15H11BrCl2N2O4S
- 化合物 T16797
- 154106-92-0
- RPR104632,RPR-104632
- 2H-1,2,4-Benzothiadiazine-3-carboxylic acid, 2-[(3-bromophenyl)methyl]-6,8-dichloro-3,4-dihydro-, 1,1-dioxide
- RPR 104632