METFORMIN BDBM50229665 1,1-Dimethylbiguanide CHEMBL1431 N,N-dimethylimidodicarbonimidic diamide
1,1-DIMETHYLBIGUANIDE HYDROCHLORIDE 3-(diaminomethylidene)-1,1-dimethylguanidine;hydrochloride 3-[bis(azanyl)methylidene]-1,1-dimethyl-guanidine;hydrochloride 3-(diaminomethylene)-1,1-dimethyl-guanidine;hydrochloride SMR000058277 Metformin MLS000028493 BDBM57047 cid_14219
- Hume, WE; Shingaki, T; Takashima, T; Hashizume, Y; Okauchi, T; Katayama, Y; Hayashinaka, E; Wada, Y; Kusuhara, H; Sugiyama, Y; Watanabe, Y The synthesis and biodistribution of [(11)C]metformin as a PET probe to study hepatobiliary transport mediated by the multi-drug and toxin extrusion transporter 1 (MATE1) in vivo. Bioorg Med Chem 21: 7584-90 (2013)
- ChEMBL_2472310 Inhibition of OCT1 (unknown origin) expressed in HEK293 cells using [14C]-metformin probe as substrate
- ChEMBL_2472311 Inhibition of OCT2 (unknown origin) expressed in HEK293 cells using [14C]-metformin probe as substrate
- ChEMBL_2472312 Inhibition of MATE1 (unknown origin) expressed in HEK293 cells using [14C]-metformin probe as substrate
- ChEMBL_2016311 (CHEMBL4669889) Inhibition of human SLC22A2 expressed in HEK293 cells in presence of para-aminohippuric acid/metformin
- ChEMBL_2016312 (CHEMBL4669890) Inhibition of human SLC22A8 expressed in HEK293 cells in presence of para-aminohippuric acid/metformin
- ChEMBL_2016313 (CHEMBL4669891) Inhibition of human SLC22A6 expressed in HEK293 cells in presence of para-aminohippuric acid/metformin
- ChEMBL_1484077 (CHEMBL3537112) Inhibition of human OCT2 expressed in MDCK2 cells using [14C]metformin as substrate by liquid scintillation counting analysis
- ChEMBL_934313 (CHEMBL2320299) Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis
- ChEMBL_934312 (CHEMBL2320298) Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis
- ChEMBL_1491730 (CHEMBL3536922) Inhibition of OCT1 (unknown origin) expressed in HEK293 cells assessed as reduction of [14C]metformin substrate uptake at 100 uM by liquid scintillation counting
- ChEMBL_1491733 (CHEMBL3536925) Inhibition of OCT2 (unknown origin) expressed in HEK293 cells assessed as reduction of [14C]metformin substrate uptake at 100 uM by liquid scintillation counting
- MATE2-K IC50 Assay MATE2-K (multidrug and toxin extrusion protein 2) is expressed in the apical membrane in the kidney and mediates the elimination of compounds to urine. MDCK-II cells were maintained in DMEM with low glucose and 10% FBS. Cells passages up to 40 were seeded at 60K±10K cells/well on 96-well, transwell membrane plates approximately 24 hours before transfection. Transport assays were carried out approximately 48 hours after transfection. On assay day, the DMEM was removed, and cells were washed with HBSS. After washing, the cells in each well were pre-incubated with HBSS containing 30 mM NH4Cl and either vehicle, the compound being tested at 6 concentrations ranging from 0.127 μM to 40 AM, or 100 μM cimetidine as a reference inhibitor. The assay plate was then placed in a 37° C. incubator with orbital shaking at approximately 60 RPM for the pre-incubation time of 15 minutes. The pre-incubation solutions were then removed, and cells washed with HBSS once. 100 μL of incubation buffer was added to each well containing HBSS with 10 μM 14[C]-metformin as the probe substrate and either vehicle control, the compound being tested (at 6 concentrations ranging from 0.127 μM to 40 μM) or reference inhibitors. The assay plate was incubated at 37° C. with orbital shaking at approximately 60 RPM for the incubation time of 5 minutes. At end of the 5-minute incubation, 15 μL of dosing solution was removed from each well containing the compound being tested and measured using LC/MS/MS for dose recovery assessment. The assay wells were then washed four times with ice cold PBS. 60 μL cell extraction solution was added to each well and the plate was incubated at 37° C. with orbital shaking at approximately 60 RPM for the 15 minutes. After this incubation, 30 μL was removed from each well, added to 200 μL scintillation fluid, and counted on a 1450 Microbeta (Perkin-Elmer) to measure the probe substrate uptake. Inhibition potential of the compound being tested was calculated by dividing the transporter-mediated uptake rate in presence of the compound being tested or the reference inhibitor by the transporter-mediated uptake rate in presence of vehicle control and fitted to a sigmoidal function to determine the IC50 values.