Phenformin HCl

製品コードS2542 バッチS254203

化学情報

	Synonyms	NSC-756501, Phenethylbiguanide	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₀H₁₅N₅.HCl
	分子量	241.72	CAS No.	834-28-6
Solubility (25°C)*	体外	DMSO	48 mg/mL (198.57 mM)
		Water	48 mg/mL (198.57 mM)
		Ethanol	48 mg/mL (198.57 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明	Phenformin HCl 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. ^[1] 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]. ^[2] 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. ^[3] 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. ^[4] Phenformin-treated rats reveals a tendency towards a decrease in blood insulin level (radioimmunoassay). ^[5]
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. ^[3]

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: Data from [Data independently produced by , , J Biol Chem, 2017, 292(7):2830-2841]

: Data from [Data independently produced by , , Biochem Biophys Res Commun, 2016, 470(2):453-459]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Quiescence enables unrestricted cell fate in naive embryonic stem cells [ Nat Commun, 2024, 15(1):1721]	PubMed: 38409226
Identification of a novel m6A-related lncRNAs signature and immunotherapeutic drug sensitivity in pancreatic adenocarcinoma [ BMC Cancer, 2024, 24(1):116]	PubMed: 38262966
Screening Health-Promoting Compounds for Their Capacity to Induce the Activity of FOXO3 [ J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493]	PubMed: 34508571
Dietary Intake Regulates the Circulating Inflammatory Monocyte Pool [ cell, 2019, 178(5):1102-1114]	PubMed: 31442403
Liquid biopsy-based single-cell metabolic phenotyping of lung cancer patients for informative diagnostics. [ Nat Commun, 2019, 10(1):3856]	PubMed: 31451693
SPARC Inhibits Metabolic Plasticity in Ovarian Cancer [ Cancers (Basel), 2018, 10(10)E385]	PubMed: 30332737
[ Oncotarget, 2017, ]	PubMed: 28938614
Serine/Threonine Kinase Unc-51-like Kinase-1 (Ulk1) Phosphorylates the Co-chaperone Cell Division Cycle Protein 37 (Cdc37) and Thereby Disrupts the Stability of Cdc37 Client Proteins. [Li R, et al. J Biol Chem, 2017, 292(7):2830-2841]	PubMed: 28073914
The epigenetic regulation of HIF-1α by SIRT1 in MPP(+) treated SH-SY5Y cells. [Dong SY, et al. Biochem Biophys Res Commun, 2016, 470(2):453-9]	PubMed: 26768367

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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