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ChemicalBook CAS数据库列表 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

生物活性靶点体外研究体内研究 3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione 试剂级价格

CAS号:941575-71-9
英文名:3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione
中文名:3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione
CBNumber:CB42695130
分子式:C21H13BrN2O3
分子量:421.24
MOL File:941575-71-9.mol

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

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 :DMSO: ≥15mg/mL
形态 :powder
酸度系数(pKa) :7.44±0.60(Predicted)
颜色 :light orange to dark orange

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 Germany :3

3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione性质、用途与生产工艺

生物活性 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。
靶点

GSK-3α

16 nM (IC ₅₀ )

GSK-3β

21 nM (IC ₅₀ )

体外研究

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.

体内研究

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.