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941575-71-9

中文名稱 3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione
CAS 941575-71-9
分子式 C21H13BrN2O3
分子量 421.244
MOL 文件 941575-71-9.mol
更新日期 2024/12/13 09:53:00
941575-71-9 結構式 941575-71-9 結構式

基本信息

中文別名
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
英文別名
BIP-135
3-(5-BroMo-1-Methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione
3-(Benzofuran-3-yl)-4-(5-bromo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione

物理化學性質(zhì)

儲存條件room temp
溶解度在DMSO中的溶解度≥15mg/mL
形態(tài)粉末
顏色淺橙色至深橙色

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS06
警示詞危險
危險性描述H301
防范說明P301+P310
危險品標志T
危險類別碼25
安全說明45
危險品運輸編號UN 2811 6.1 / PGIII
WGK Germany3

常見問題列表

生物活性
BIP-135 是一個高效、選擇性的,ATP 競爭性的 GSK-3 抑制劑,對 GSK-3α 和 GSK-3β 作用的IC50 值分別為 16 nM 和 21 nM。BIP 135 具有神經(jīng)保護作用。
靶點

GSK-3α

16 nM (IC 50 )

GSK-3β

21 nM (IC 50 )

體外研究

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.
體內(nèi)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.
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