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KI0796Metformin hydrochloride50 mg$154

Chemical Characteristic

Product NameMetformin hydrochloride
SynonymsGlucophage, Glucophage XR, Riomet
CAS No.1115-70-4
Molecular Weight 165.62
FormulaC4H12ClN5
Chemical Structure

Biological activities

Metformin hydrochloride is a hydrochloride salt of metformin. Metformin is an oral antidiabetic agent in the biguanide class. Metformin dose-dependently increases glucose uptake and the following lactate production at 30 to 100 µM.[1] The IC50 of metformin is 21 and 18 µM against ishikawa and HEC-1B cells, respectively. Metformin enhances the antitumor effect of medroxyprogesterone acetate (MPA) using ishikawa and HEC-1B EC cell lines. Metformin markedly promotes progesterone receptor expression. Metformin increases AMPK (AMP-activated protein kinase) phosphorylation and decreases p70S6K phosphorylation.[2] Metformin with insulin significantly increases mRNA expressions of INSR, IGF-1R, and IRS-1.[3] Antidiabetic actions of metformin involve the reduction of hepatic glucose production and/or insulin resistance. Metformin inhibits DPP IV activity present in mouse plasma with IC50 of 38 µM and 29 µM for normal mice and ob/ob mice, respectively.[4] Metformin decreases plasma glucose more in a fed state than in a fasted state in GK rats.[1] Long-term (12 day) oral metformin administration to ob/ob mice results in lower DPP IV activity but has no effect on basal glucose and insulin levels.[4] When mice are given metformin, the blood lactate concentration significantly increases in the wild-type mice, whereas only a slight increase is observed in Oct1(-/-) mice.[5]

Protocols

In vivo: Metformin is dissolved in saline.[5]

References

[1] Yoshida T, et al. Metformin primarily decreases plasma glucose not by gluconeogenesis suppression but by activating glucose utilization in a non-obese type 2 diabetes Goto-Kakizaki rats. Eur J Pharmacol. 2009, 623(1-3): 141-147.
[2] Xie Y, et al. Metformin promotes progesterone receptor expression via inhibition of mammalian target of rapamycin (mTOR) in endometrial cancer cells. J Steroid Biochem Mol Biol. 2011, 126(3-5): 113-120. 閵嗏偓閵嗏偓
[3] Lee MS, et al. Metformin enhances the action of insulin on porcine granulosa-lutein cells in vitro. Anim Reprod Sci. 2012, 136(1-2): 100-107. 閵嗏偓閵嗏偓
[4] Green BD, et al. Inhibition of dipeptidyl peptidase-IV activity by metformin enhances the antidiabetic effects of glucagon-like peptide-1. Eur J Pharmacol. 2006, 547(1-3): 192-199. 閵嗏偓閵嗏偓
[5] Wang DS, et al. Involvement of organic cation transporter 1 in the lactic acidosis caused by metformin. Mol Pharmacol. 2003, 63(4): 844-848. 閵嗏偓閵嗏偓

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