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692-13-7

中文名稱 丁福明
英文名稱 1-butylbiguanide
CAS 692-13-7
分子式 C6H15N5
分子量 157.217
MOL 文件 692-13-7.mol
692-13-7 結(jié)構(gòu)式 692-13-7 結(jié)構(gòu)式

基本信息

中文別名
丁福明
英文別名
DBV
W 37
H 224
Glybigid
Buformin
Butformin
Buformine
Dibetos B
Butyldiguanide
Butylbiguanide
所屬類別
原料藥:胰腺激素及其它調(diào)節(jié)血糖藥

物理化學(xué)性質(zhì)

沸點(diǎn)271.89°C (rough estimate)
密度1.0291 (rough estimate)
折射率1.8070 (estimate)

常見問題列表

生物活性
Buformin (1-Butylbiguanide) 是一種有效的 AMPK 活化劑,也是具有口服活性的雙胍類降血糖試劑 (antidiabetic agent)。Buformin 降低肝糖異生并降低血糖生成。Buformin 也具有抗癌活性,可以應(yīng)用于癌癥研究,如宮頸癌、乳腺癌等。
體外研究

Buformin (0-10?mM; 5 days) inhibits SKBR3 and BT474 cells growth as a concentration-dependent manner, exhibits IC 50 values of 246.7?μM and ?98.6?μM for erbB-2-overexpressing SKBR3 and BT474 cells, respectively.Buformin (0-3 mM; 48 hours) ?increases the percentage of cells in G0/G1 phase and reduced the percentage of cells in S phase, especially in the SKBR3 cells.Buformin (0-3 mM; 24 hours) suppresses RTK activation, including erbB-2 and IGF1R signaling ?downstream, and Akt activation/phosphorylation is inhibited in both SKBR3 and BT474 cells.

Cell Viability Assay

Cell Line: ErbB-2-overexpressing SKBR3 and BT474 cells
Concentration: 0 μM, 1 μM, 3 μM, 10 μM, 30 μM, 100 μM, 300?μM, 1, 3, or 10?mM
Incubation Time: 5 days
Result: Reduced cell viability in erbB-2-overexpressing breast cells.

Cell Cycle Analysis

Cell Line: ErbB-2-overexpressing SKBR3 and BT474 cells
Concentration: 0.5 mM; 1 mM; 3 mM
Incubation Time: 48 hours
Result: Increased cells arresting in G0/G1 phase.

Western Blot Analysis

Cell Line: ErbB-2-overexpressing SKBR3 and BT474 cells
Concentration: 0?mM, 0.1?mM, 0.3?mM, 1?mM, or 3?mM
Incubation Time: 24 hours
Result: Decreased p-AMPK, p-p706S, p-ERK1/2 expression in a concentration-dependent manner.
體內(nèi)研究

Buformin (oral administation; 7.6?mmol/kg of chow; 7 days) exhibits significantly reduced tumor volumes and weights, and?hinders mammary morphogenesis and proliferation in MMTV-erbB-2 transgenic mice

Animal Model: Female MMTV-erbB-2 transgenic mice
Dosage: 7.6?mmol/kg
Administration: Oral administation; 7 days
Result: Inhibited mammary syngeneic tumor growth in MMTV-erbB-2 transgenic mice.
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