丁双胍盐酸盐 Buformin hydrochloride CAS#:1190-53-0

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首页化工产品目录原料药激素及调节内分泌功能类药胰腺激素及其它调节血糖药丁双胍盐酸盐

丁双胍盐酸盐

产品纠错

CAS号：1190-53-0 | 英文名称：Buformin hydrochloride

分子式 C₆H₁₆ClN₅

分子量 194

EINECS号 214-723-6

MDL MFCD00045591

Smiles

InChIKey

乙二醇化学百科

基本信息

中文名称	盐酸丁双胍
英文名称	BuforMin Hydrochloride
CAS号	1190-53-0
分子式	C6H16ClN5
分子量	193.68
EINECS号	214-723-6

物化性质

熔点	177-179?C
溶解度	DMSO（少许）、甲醇（少许）、水（少许）
形态	固体
颜色	白色至类白色
稳定性	吸湿性

安全信息

危险类别码	22-43-36
安全说明	36/39-46
海关编码	29212900
毒性	LD50 i.p. in mice: 380 mg/kg (Rikimaru)

生产及用途

生物活性

Buformin hydrochloride (1-Butylbiguanide hydrochloride) 是一种有效的 AMPK 活化剂，也是具有口服活性的双胍类降血糖试剂 (antidiabetic agent)。Buformin 降低肝糖异生并降低血糖生成。Buformin 也具有抗癌活性，可以应用于癌症研究，如宫颈癌、乳腺癌等。

体外研究

Buformin hydrochloride (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 hydrochloride (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 hydrochloride (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.

体内研究

Buformin hydrochloride (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.