Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. Glibenclamide can also induce autophagy.
Glibenclamide (2 mg/kg; p.o.) increases of insulin release and rapid drop of blood glucose level in mice.
|Solubility (25°C)||DMSO > 100 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Olezarsen, an N-acetylgalactosamine (GalNAc)-suffixed antisense oligonucleotide (ASO) targeting hepatic APOC3 mRNA, inhibits the production of apolipoprotein C-III (apoC-III) and can be used in studies related to familial celiac sprue syndrome (FCS).
Lumasiran is a siRNA compound that reduces hepatic oxalate production by targeting ethanoic acid oxidase.
Givosiran is a small interfering RNA that targets hepatic aminofibrillar synthase 1 (ALAS1) messenger RNA, down-regulates ALAS1 mRNA, and prevents the accumulation of neurotoxic Î±-aminofibrillar acids and porphyrins, which can be used in porphyria-related studies.
Viltolarsen is a phosphorodiamidomorpholine antisense oligonucleotide that targets splicing of exon 53 of the myotonic dystrophy protein gene and can be used in the study of Duchenne muscular dystrophy (DMD).
Golodirsen is a phosphodiesteric morpholino oligomer (PMO) that specifically targets exon 53 of the pre-protein mRNA of myotonic dystrophy protein culture proteins, and can be used in studies related to Duchenne muscular dystrophy (DMD).
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