Name | phenformin hydrochloride |
Synonyms | 1-Phen meltrol PHENFORMIN HCL Phenformine HCL phenformin hydrochloride 1-Fenetilbiguanide cloridrato [Italian] 1-(diaminomethylene)-2-phenethylguanidine hydrochloride 1-(diaminomethylene)-2-phenethyl-guanidine hydrochloride 1-(diaminomethylidene)-2-phenethylguanidine hydrochloride 1-(diaminomethylidene)-2-phenethyl-guanidine hydrochloride n-(2-phenylethyl)-imidodicarbonimidicdiamidmonohydrochloride |
CAS | 834-28-6 |
EINECS | 212-637-3 |
InChI | InChI=1/C10H15N5.ClH/c11-9(12)15-10(13)14-7-6-8-4-2-1-3-5-8;/h1-5H,6-7H2,(H6,11,12,13,14,15);1H |
Molecular Formula | C10H16ClN5 |
Molar Mass | 241.72 |
Melting Point | 175-178°C |
Boling Point | 413.7°C at 760 mmHg |
Flash Point | 204°C |
Water Solubility | >=10 g/100 mL at 21 ºC |
Solubility | Methanol (Slightly), Water (Slightly) |
Vapor Presure | 4.71E-07mmHg at 25°C |
Appearance | neat |
Color | White to Off-White |
Storage Condition | Keep in dark place,Inert atmosphere,2-8°C |
MDL | MFCD00035039 |
Use | Used as a hypoglycemic agent |
In vitro study | Phenformin stimulates the phosphorylation and activation of AMPKalpha1 and AMPKalpha2 without altering the activity of the LKB1 gene. In the isolated heart, Phenformin increased AMPK activity and phosphorylation, and increased AMPK activity and increased intracellular [AMP] correlated. Phenformin is 50 times more potent than metformin and inhibits mitochondrial complex I. Phenformin induces apoptosis in LKB1 null non-small cell lung cancer cell lines. Phenformin(2 mM) also induced AMPK signaling, increasing the levels of P-AMPK and P-Raptor. Phenformin causes higher levels of cellular stress, triggering the induction of P-Ser51 eIF2α and its downstream target CHOP, a molecular marker for later apoptosis. In chronically treated KLluc mice, Phenformin induced survival and response to treatment. In H441 cells, Phenformin and AICAR increased AMPK activity in a dose-dependent manner, maximally stimulating kinase by 5-10 mM and 2 mM, respectively. In H441 monolayers, Phenformin significantly reduced basal ion migration (measured as short circuit current) by about 50%. Compared with the control group, Phenformin and AICAR significantly reduced amiloride-sensitive transmembrane Na ion transport. Phenformin and AICAR inhibit amiloride-sensitive transmembrane Na ion transport in H441 cells by inducing the activation of AMPK and inducing terminal and basolateral sodium ions through Na, inhibition of K ATP enzyme entry into ENaC cells. Phenformin-treated rats showed a tendency to decrease insulin levels in their blood (radioimmunoassay). |
In vivo study | Phenformin also increased the levels of P-eIF2α and its target BiP/ Grp78 in normal lung as well as in lung tumors in mice. |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
Safety Description | 36 - Wear suitable protective clothing. |
WGK Germany | 3 |
RTECS | DU2200000 |
HS Code | 29252900 |
Toxicity | LD50 in mice (mg/kg): 19 i.v., 450 orally; in rats: 1050 orally; in guinea pigs: 47 orally, 19 s.c. (Proske) |
This product is l-(2-phenylethyl) biguanide hydrochloride. The content of C10H15N5 • HC1 shall not be less than 99.0% calculated on a dry basis.
The melting point of this product (General 0612) is 174~178°C.
take 0.20g of this product, Add 10ml of water to dissolve, and measure according to law (General rule 0631). The pH value should be 6.0~7.0.
take this product l. Add methanol to dissolve in 10ml measuring flask, dilute to the scale, shake well, test by paper chromatography (General rule 0501), draw 0.2 accurately, point on two chromatographic filter paper strips (7.5cm × 50cm) respectively, and use methanol as blank point on the other chromatographic filter paper strip, the sample point diameter is 0.5 ~ 1cm; According to the descending method, the above chromatographic filter paper strips were spread in the same chamber, using ethyl acetate-ethanol-water (6:3:1) as the spreading solvent, and spread to the front about 7cm from the lower end, take out, dry, use color reagent (take 10% potassium ferricyanide solution 1ml, add 10% sodium nitroprusside solution and 10% sodium hydroxide solution 1ml, shake, place for 15 minutes, add water 10ml and acetone 12ml, mix well) spray one of the spotting strips (about biguanide red band, the private value is about 0.1), refer to this band, on the other spotting strip and blank strip, cut the corresponding parts and extend out for 1cm, and cut them into broken strips. Take 20ml of each methanol for precision measurement, and extract them separately according to UV-Vis spectrophotometry (General rule 0401), absorbance was measured at a wavelength of 232nm. 48.
take this product, dry to constant weight at 105°C, weight loss shall not exceed 1.0% (General rule 0831).
not over 0841 (general rule).
take this product about 0.lg, precision weighing, add glacial acetic acid 20ml to dissolve, add acetic anhydride 20ml, according to the potentiometric titration method (General rule 0701), with perchloric acid titration solution (O. 1 mol/L) titration, and the results of the titration were corrected with a blank test. Each 1 ml of perchloric acid titration solution (0.1 mol/L) corresponds to 12.09mg of Cl0H15N5. Hc1.
hypoglycemic drugs.
sealed storage.
This product contains phenformin hydrochloride (C10H15N5 • HCI) should be labeled 90.0% ~ 110.0%.
This product is white tablet.
should be in accordance with the relevant provisions under The tablet item (General rule 0101).
with phenformin hydrochloride.
25mg
sealed storage.