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42494-73-5

CAS 42494-73-5
42494-73-5 結(jié)構(gòu)式 42494-73-5 結(jié)構(gòu)式

物理化學(xué)性質(zhì)

儲存條件-20°C
溶解度在水中的溶解度為20mg/mL,澄清
形態(tài)黃色固體
顏色淡黃色至深黃色

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H315-H319-H335
危險品標志Xi
危險類別碼36/37/38
安全說明36/37/39
WGK Germany3

常見問題列表

生物活性
bpV(phen),一種胰島素模擬物,是一種有效的蛋白酪氨酸磷酸酶 (PTP) 和 PTEN 抑制劑,對 PTEN,PTP-β 和 PTP-1B 的 IC50 為 38 nM,343 nM 和 920 nM。bpV(phen) 在體外抑制原生動物寄生蟲利什曼原蟲的增殖。bpV(phen) 強烈誘導(dǎo)大量趨化因子和促炎性細胞因子的分泌,并激活 Th1 型途徑 (IL-12,IFNγ)。bpV(phen) 還可以誘導(dǎo)細胞凋亡 (apoptosis),并具有抗血管生成和抗腫瘤活性。
靶點

IC50: 38 nM (PTEN), 343 nM (PTP-β) and 920 nM (PTP-1B)
Parasite Leishmania
Apoptosis

體外研究

bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment causes a further decrease of cell viability in H/R-injured H9c2 cells.
bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment increases the apoptosis of H/R-injured H9c2 cells.
bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment significantly promotes the accumulation of cytoplasmic Cytochrome C in H/R-injured H9c2 cells.
After stimulation of bpV(phen), PTEN-induced putative kinase protein 1 (PINK1)/Parkin-mediated mitophagy is inhibited.
bpV(phen) is an insulin-mimetic agent following insulin-receptor tyrosine kinase hyperphosphorylation and activation.

Cell Viability Assay

Cell Line: Hypoxia/reoxygenation (H/R)-injured H9c2 cells
Concentration: 5 μM
Incubation Time: 24.5 hours (hypoxia for 24 h; reoxygenation for 30 minutes)
Result: Caused a further decrease of cell viability.

Apoptosis Analysis

Cell Line: Hypoxia/reoxygenation (H/R)-injured H9c2 cells
Concentration: 5 μM
Incubation Time: 24.5 hours (hypoxia for 24 h; reoxygenation for 30 minutes)
Result: Increased the apoptosis of H/R-injured H9c2 cells.

Western Blot Analysis

Cell Line: Hypoxia/reoxygenation (H/R)-injured H9c2 cells
Concentration: 5 μM
Incubation Time: 24.5 hours (hypoxia for 24 h; reoxygenation for 30 minutes)
Result: Showed an increased release of Cytochrome C.
體內(nèi)研究

bpV(phen) (5 mg/kg; intraperitoneal injection; daily; for 38 days; male BALB/c nude (nu/nu) athymic mice) treatment causes a significant reduction in average tumor volume.

Animal Model: Male BALB/c nude (nu/nu) athymic mice (6-7 weeks old) injected with PC-3 cells
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; daily; for 38 days
Result: Caused a significant reduction in average tumor volume.
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