3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione

3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione

中文名称3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione
中文同义词3-(苯并呋喃-3-基)-4-(5-溴-1-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮;化合物 T14613;化合物BIP-135
英文名称3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione
英文同义词3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione;BIP-135;3-(Benzofuran-3-yl)-4-(5-bromo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione;BIP 135,BIP135;1H-Pyrrole-2,5-dione, 3-(3-benzofuranyl)-4-(5-bromo-1-methyl-1H-indol-3-yl)-
CAS号941575-71-9
分子式C21H13BrN2O3
分子量421.24
EINECS号
相关类别Aromatics, Pharmaceuticals, Intermediates & Fine Chemicals
Mol文件941575-71-9.mol
结构式3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione 结构式

3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione 性质

沸点643.5±55.0 °C(Predicted)
密度1?+-.0.1 g/cm3(Predicted)
储存条件room temp
溶解度在DMSO中的溶解度≥15mg/mL
形态粉末
酸度系数(pKa)7.44±0.60(Predicted)
颜色浅橙色至深橙色粘性

3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione 用途与合成方法

BIP-135 是一个高效、选择性的,ATP 竞争性的 GSK-3 抑制剂,对 GSK-3α 和 GSK-3β 作用的IC50 值分别为 16 nM 和 21 nM。BIP 135 具有神经保护作用。

GSK-3α

16 nM (IC 50 )

GSK-3β

21 nM (IC 50 )

BIP-135 (20-30 μM; 72 hours) increases the survival motor neuron (SMN) protein levels at a dose of 25 μM in human SMA fibroblasts. And the typical bell-shaped dose-response curve is observed due to some toxicity at higher concentrations.
BIP-135 (20 μM; 48 hours) is a superior neuroprotective agent in the model of oxidative stress.

Western Blot Analysis

Cell Line: Human SMA fibroblasts
Concentration: 20 μM, 25 μM, 30 μM
Incubation Time: 72 hours
Result: Led to a 7-fold increase in SMN levels at 25 μM.

BIP-135 does not appear to be toxic and was well-tolerated by the animals (no decrease in body weight).
BIP-135 (75 mg/kg; i.p.; daily; from postnatal day 0 to 21) prolongs the median survival time of Δ7 SMA KO mouse model of spinal muscular atrophy.

Animal Model: Male and female SMN2 +/+ , SMN2Δ7 +/+ , Smn +/– mice
Dosage: 75 mg/kg
Administration: Intraperitoneal injection; daily; from postnatal day 0 to 21
Result: Caused a modest extension in the median survival of SMA KO animals by two days.

安全信息

危险品标志T
危险类别码25
安全说明45
危险品运输编号UN 2811 6.1 / PGIII
WGK Germany3

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-1110553-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione
BIP-135
941575-71-91mg681元
2024/04/30HY-1110553-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione
BIP-135
941575-71-910mg2400元

3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione 上下游产品信息

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