1,1-Dimethylbiguanide, Hydrochloride A antihyperglycemic biguanide which stimulates AMPK

1,1-Dimethylbiguanide, Hydrochloride  (CAS 1115-70-4)

1,1-Dimethylbiguanide, Hydrochloride | CAS 1115-70-4 is rated 5.0 out of 5 by 1.
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| See product citations (5)
Synonym: Metformin hydrochloride
Application: A antihyperglycemic biguanide which stimulates AMPK
CAS Number: 1115-70-4
Purity: ≥99%
Molecular Weight: 165.62
Molecular Formula: C4H11N5•HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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Ordering Information

1,1-Dimethylbiguanide, Hydrochloride sc-202000 1 g $20.00
1,1-Dimethylbiguanide, Hydrochloride sc-202000A 5 g $31.00

1,1-Dimethylbiguanide, Hydrochloride (Metformin) is a biguanide antihyperglycemic agent. Through glucose clamp investigation in rats 1,1-Dimethylbiguanide, Hydrochloride has been shown to lower blood glucose levels through improved glucose tolerance without stimulating insulin secretion, promoting weight gain or causing hypoglycemia. The biguanide reduces the diabetic complications on the cardiovascular system and increases insulin sensitivity. The compound has been shown not to change the synthesis of either GLUT4 or GLUT1 but does stimulate the transport of GLUT1 to the plasma membrane as seen in skeletal muscles. The compound has also been observed to improve peripheral arterials through selective reduction of PAI-1 (plasminogen activator inhibitor). In Xenopus oocytes the compound has been documented to act by increasing intercellular calcium concentration in addition to elevating receptor tyrosine kinase activity and inositol 1,4,5-trisphosphate. 1,1-Dimethylbiguanide, Hydrochloride has demonstrated the ability to induce fatty acid oxidation and to stimulate AMP-activated protein kinase (AMPK) leading to the reduction in acetyl-CoA carboxylase activity. In brown adipocytes 1,1-Dimethylbiguanide, Hydrochloride has been observed to inhibit leptin secretion via a mitogen-activated protein kinase signalling pathway.


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Appearance :
Physical State :
Solubility :
Soluble in water (50 mg/ml), ethanol, and DMSO (50 mM).
Storage :
Store at 4° C
Melting Point :
223-226° C (lit.)
Boiling Point :
224.1° C at 760 mmHg
IC50 :
Streptococcus sp. 'group A': EC5050 = 4.08 µM; Streptokinase A: EC5050 = 5.65 µM (Streptococcus pyogenes serotype M1)
pK Values :
pKb: 12.25 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
PubChem CID :
Merck Index :
14: 5938
MDL Number :
EC Number :

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Certificate of Analysis

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1,1-Dimethylbiguanide, Hydrochloride Product Citations

See how others have used 1,1-Dimethylbiguanide, Hydrochloride. Click on the entry to view the PubMed entry .

Citations 1 to 5 of 5 total

PMID: # 28243322
García-Castillo, V. et al. 2017. Targeting Metabolic Remodeling in Triple Negative Breast Cancer in a Murine Model. J Cancer. 8: 178-189.

PMID: # 26771051
Kinsky, OR. et al. 2016. Metformin Scavenges Methylglyoxal To Form a Novel Imidazolinone Metabolite in Humans. Chemical research in toxicology.

PMID: # 11994296
Fryer, LG. et al. 2002. The Anti-diabetic drugs rosiglitazone and metformin stimulate AMP-activated protein kinase through distinct signaling pathways. J. Biol. Chem.. 277: 25226-25232.

PMID: # 11602624
Zhou, G. et al. 2001. Role of AMP-activated protein kinase in mechanism of metformin action. J. Clin. Invest.. 108: 1167-1174.

PMID: # 9428832
Garber, AJ. et al. 1997. Efficacy of metformin in type II diabetes: results of a double-blind, placebo-controlled, dose-response trial. Am. J. Med.. 103: 491-497.

Citations 1 to 5 of 5 total
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Rated 5 out of 5 by from Fryer et al Fryer et al. (PubMed ID 11994296) used 1,1-Dimethylbiguanide, Hydrochloride (metformin hydrochloride) to activate AMPK in hepatocytes without having to increase AMP:ATP ratios. -SCBT Publication Review
Date published: 2015-03-09
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