计算溶液所需的质量、体积或浓度。
概述
Phenformin hydrochloride 是一种双胍类的抗糖尿病剂，能够使 AMPK 活化。
Information
Phenformin (NSC-756501) HCl Phenformin HCl (NSC-756501, Phenethylbiguanide) is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class. It activates AMPK , increasing activity and phosphorylation.
In vitro
Phenformin stimulates the phosphorylation and activation of AMPKalpha1 and AMPKalpha2 without altering LKB1 activity. Phenformin increases AMPK activity and phosphorylation in the isolated heart, the increase in AMPK activity is always preceded by and correlated with increased cytosolic [AMP]. Phenformin is a 50-fold more potent inhibitor of mitochondrial complex I than metformin. Phenformin robustly induces apoptosis in LKB1 deficient NSCLC cell lines. Phenformin at 2 mM similarly induces AMPK signaling as shown by increased P-AMPK and P-Raptor levels. Phenformin induces higher levels of cellular stress, triggering induction of P-Ser51 eIF2α and its downstream target CHOP, and markers of apoptosis at later times. Phenformin induces a significant increase in survival and therapeutic response in KLluc mice following long-term treatment. Phenformin and AICAR increases AMPK activity in H441 cells in a dose-dependent fashion, stimulating the kinase maximally at 5-10 mm and 2 mm, respectively. Phenformin significantly decreases basal ion transport (measured as short circuit current) across H441 monolayers by approximately 50% compared with that of controls. Phenformin and AICAR significantly reduce amiloride-sensitive transepithelial Na+ transport compared with controls. Phenformin and AICAR suppress amiloride-sensitive Na+ transport across H441 cells via a pathway that includes activation of AMPK and inhibition of both apical Na+ entry through ENaC and basolateral Na+ extrusion via the Na+,K+-ATPase. Phenformin-treated rats reveals a tendency towards a decrease in blood insulin level (radioimmunoassay).
In vivo
Phenformin also increases levels of P-eIF2α and its target BiP/Grp78 in normal lung as well as in lung tumors of mice.
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥96%
规格
英文别名
Phenethylbiguanide HCl
规格或纯度
10mM in DMSO
英文名称
Phenformin (NSC-756501) HCl
生化机理
盐酸苯乙双胍（NSC-756501，Phenethylbiguanide）是苯乙双胍的盐酸盐，属于双胍类抗糖尿病药物。它能激活 AMPK，增加其活性和磷酸化。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
EC号
212-637-3
分子类型
小分子
Isomeric SMILES
C1=CC=C(C=C1)CCN=C(N)N=C(N)N.Cl
UN Number
Packing Group
I
分子量
241.72
Reaxy-Rn
35474258
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=35474258&ln=
高级数据
安全和危险性（GHS）
信号词
警告
危险声明
H227: 可燃液体
预防措施声明
P210: 远离热源，热表面，火花，明火和其他点火源。 - 禁止抽烟。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P370+P378: 火灾时：使用干砂、干粉或抗醇泡沫灭火。
P403+P235: 存放在通风良好的地方。保持低温。
P501: 将内容物/容器送到批准的废物处理厂处理
WGK Germany
3
RTECS
DU2200000
Class
6.1
个人防护装备
dust mask type N95 (US),Eyeshields,Gloves
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 C2307021 |
分析证书 | P408094 |
此产品的引用文献
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 834-28-6，分子式为 C10H15N5 · HCl，分子量为 241.72 g/mol。
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