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Glibenclamide

Cat. No. M3547
Glibenclamide Structure
Synonym:

Glyburide; RP-1127; BIIB093

Size Price Availability Quantity
Free Sample (1-2 mg)  USD 0 In stock
500mg USD 51  USD51 In stock
1g USD 65  USD65 In stock
5g USD 77  USD77 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 494
Formula C23H28ClN3O5S
CAS Number 10238-21-8
Solubility (25°C) DMSO > 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

References

[1] Żaneta Kimber-Trojnar, et al. Is glyburide safe in pregnancy?

[2] Selvan Ravindran, et al. Metabolic profile of glyburide in human liver microsomes using LC-DAD-Q-TRAP-MS/MS

[3] Olga L Zharikova, et al. Kinetics of glyburide metabolism by hepatic and placental microsomes of human and baboon

[4] L P Krall. Glyburide (DiaBeta): a new second-generation hypoglycemic agent

[5] G F Peart, et al. The metabolism of glyburide in subjects of known debrisoquin phenotype

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  Catalog
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Keywords: Glibenclamide, Glyburide; RP-1127; BIIB093 supplier, inhibitors, activators


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