Free shipping on all orders over $ 500

Phenformin HCl

Cat. No. M5336
Phenformin HCl Structure

Phenethylbiguanide hydrochloride

Size Price Availability Quantity
500mg USD 50  USD50 In stock
1g USD 60  USD60 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 241.72
Formula C10H15N5.HCl
CAS Number 834-28-6
Purity 99.65%
Solubility 38 mg/mL in DMSO
Storage at -20°C

[1] Geldermans CA, et al. Diabetologia. The effect of phenformin-HCl on patients with diabetes mellitus, studied under strict balance conditions.

Related AMPK Products

IM156, a metformin derivative, is an oxidative phosphorylation inhibitor that increases AMPK phosphorylation.


MK-3903 is a potent and selective AMPK activator (EC50 = 8 nM).


PF-06409577 is a potent and selective activator of 5′ adenosine monophosphate-activated protein kinase (AMPK).


HTH-01-015 is a potent and selective NUAK1 inhibitor with IC50 of 100 nM, >100-fold selectivity over NUAK2.

Bempedoic acid (ETC-1002)

Bempedoic acid (ETC-1002) is a novel, first-in-class, orally available ATP-citrate lyase (ACL) inhibitor, Bempedoic acid (ETC-1002) can activate AMPK.

Abmole Inhibitor Catalog 2017

Keywords: Phenformin HCl, Phenethylbiguanide hydrochloride supplier, AMPK, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.