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Product Name:Phenformin Hydrochloride 

Synonyms:1-(diaminomethylene)-2-phenethylguanidine hydrochloride;1-(diaminomethylene)-2-phenethyl-guanidine hydrochloride;1-(diaminomethylidene)-2-phenethylguanidine hydrochloride;1-(diaminomethylidene)-2-phenethyl-guanidine hydrochloride;1-Fenetilbiguanide cloridrato [Italian];1-Phen;PHENFORMIN HCL;PHENFORMIN HYDROCHLORIDE

CAS:834-28-6

MF:C10H16ClN5

MW:241.72

EINECS:212-637-3

Appearance:White Powder

Usage It is an anti-diabetic drug from the biguanide class

Usage erectile dysfunction therapy

Description

Phenformin is an antidiabetic drug from the biguanide class. It was marketed as DBI by Ciba-Geigy, but was withdrawn from most markets in the late 1970s due to a high risk of lactic acidosis, which was fatal in 50% of cases.

Phenformin was discovered in 1957 by Ungar, Freedman and Seymour Shapiro, working for the US Vitamin Corporation. Clinical trials begun in 1958 showed it to be effective, but with gastrointestinal side effects.

Chemistry and pharmacokinetics

Phenformin hydrochloride is a white crystalline powder, with a melting point of 175 to 178 °C; it is soluble at 1 in 8 parts of water and 1 in 15 of ethanol, and practically insoluble in chloroform and ether. Phenformin is less polar and more lipid soluble and exhibits a higher affinity for mitochondrial membranes than metformin.[8] Its dissociation constant (pKa) is 2.7, 11.8 (at 32 °C), and partition coefficient (log P in octanol/water) = -0.8.[citation needed]

Phenformin is well absorbed after oral administration. The major metabolic reaction is aromatic hydroxylation to form 4-hydroxyphenformin, which is then conjugated with glucuronic acid. Up to about 50% of a dose is excreted in the urine in 24 h, about two-thirds in the form of unchanged drug and one-third as the hydroxy metabolite. Following a single oral dose of 50 mg to eight subjects, peak plasma concentrations of 0.08 to 0.18 mg/l (mean 0.13) were attained in about 3 h; plasma concentrations were higher in four subjects who were poor metabolisers of debrisoquine in comparison with the four extensive metabolisers. Following daily oral doses of 50 mg three times a day to 8 subjects, plasma concentrations of 0.10 to 0.24 mg/l (mean 0.18) were reported 2 h after a dose. Plasma half-life of phenformin is 10 to 15 h. Phenformin protein binding in plasma is about 12 to 20%.

Usage

1.Usage It is an anti-diabetic drug from the biguanide class 

2.Usage erectile dysfunction therapy 

General Description White solid or powder. Formerly used as an anti-diabetic drug. Toxic (causes lactic acidosis. Air & Water Reactions Water soluble. 

Reactivity Profile Phenformin hydrochloride gives weakly acidic aqueous solutions. May react with strong oxidizing agents. 

Fire Hazard Flash point data for Phenformin hydrochloride are not available; however,Phenformin hydrochloride is probably combustible. 

Indications: for the patients with type 2 diabetes simple diet control is not satisfactory, especially with obesity and hyperinsulinemia, use of the product not only has the effect of reducing blood sugar, may also help reduce weight and hyperinsulinemia effect.

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