e-Drug3D

739

ACARBOSE

INN
ACARBOSE

cas 56180-94-0

CLASS

METABOLISM
MEMBRANE-BOUND INTESTINAL ALPHA-GLUCOSIDE HYDROLASE INHIBITOR
HYPOGLYCEMIC AGENTS
DELAYS THE DIGESTION OF INGESTED CARBOHYDRATES
PANCREATIC ALPHA-AMYLASE INHIBITOR

ROUTE (list)

ORAL

ATC code

A10BF01
A10BD17

PK parameters

F 2 PERCENT
Tmax 1 HOUR
VD 20.8 LITER (65 KILOGRAM)
Cl 8.5 LITER / HOUR (65 KILOGRAM)
t1/2 2 HOUR

Solubility

SOLUBLE IN WATER

Target

TARGET LYSOSOMAL ALPHA-GLUCOSIDASE
PANCREATIC ALPHA-AMYLASE

PDB
5HQA (A GLYCOSIDE HYDROLASE FAMILY 97 ENZYME IN COMPLEX WITH ACARBOSE FROM PSEUDOALTEROMONAS SP. STRAIN K8)

Ligand code = ACR (link to the list of PDB complexes)

Download experimental 3D coordinates of ACR with added hydrogens

DrugCentral

Maltase-glucoamylase, intestinal UNIPROT O43451 MGAM

Pancreatic alpha-amylase UNIPROT P04746 AMY2A

Download SDF file

(2R,3R,4R,5S,6R)-5-[(2R,3R,4R,5S,6R)-5-[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-[[(1S,4S,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-1-cyclohex-2-enyl]amino]oxan-2-yl]oxy-3,4-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-6-(hydroxymethyl)oxane-2,3,4-triol

Formula:
C25H43NO18

Calculated chemical properties:

MW 645.60
NB_atoms 44
XLogP -8.56
PSA 313.947
NB_HD 14
NB_HA 19
fsp3 0.92
Lipinski(0=no;1=yes) 0

FDA
NDA 020482 (label) INN (ACARBOSE) PRECOSE (BAYER HLTHCARE) APPROVAL= AP YEAR= 1995 DISCONTINUED
NDA 077532 (pdf not found) INN (ACARBOSE) ACARBOSE (WATSON LABS) APPROVAL= AP YEAR= 2008
NDA 078470 (pdf not found) INN (ACARBOSE) ACARBOSE (HIKMA) APPROVAL= AP YEAR= 2008
NDA 078441 (pdf not found) INN (ACARBOSE) ACARBOSE (IMPAX LABS) APPROVAL= AP YEAR= 2009
NDA 091053 (pdf not found) INN (ACARBOSE) ACARBOSE (DASH PHARMS) APPROVAL= AP YEAR= 2011 DISCONTINUED
NDA 090912 (pdf not found) INN (ACARBOSE) ACARBOSE (STRIDES PHARMA) APPROVAL= AP YEAR= 2011
NDA 202271 (pdf not found) INN (ACARBOSE) ACARBOSE (AVET LIFESCIENCES) APPROVAL= AP YEAR= 2012
NDA 091343 (pdf not found) INN (ACARBOSE) ACARBOSE (SOMERSET THERAPS LLC) APPROVAL= AP YEAR= 2013
NDA 213821 (pdf not found) INN (ACARBOSE) ACARBOSE (HANGZHOU ZHONGMEI) APPROVAL= AP YEAR= 2020 DISCONTINUED