General
Preferred name
REPAGLINIDE
Synonyms
CHEMBL1272 ()
AG-EE 623ZW ()
AG-EE 388 ZW ()
AG-EE 623 ZW ()
Novonorm ()
A10BX02 ()
Enyglid ()
Prandin ()
NSC-759893 ()
AG-EE-623-ZW ()
AG-EE-623ZW ()
AGEE-623ZW ()
Repaglinide-d5 ()
P&D ID
PD000219
CAS
135062-02-1
1217709-85-7
Tags
probe
natural product
drug
available
Approved by
FDA
First approval
1997
Drug Status
investigational
approved
Drug indication
Diabetic complication
Max Phase
Phase 4
Probe info
Probe type
calculated probe
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
1
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
COMMENT
Repaglinide is a member of the meglitinide family of insulin secretagogues. Like the sulfonylurea class of anti-diabetes drugs, Repaglinide binds and inhibits the KATP (ATP-dependent potassium channel) in beta cells, causing membrane depolarization, calcium influx, and insulin secretion. The meglitinides, however, have slightly different biophysical interactions with the channel, and are more optimized for clinical use than for investigation as a probe in cell culture. If one is studying the KATP channel itself and insulin secretion in cells, the sulfonylureas seem to be quite good probes already, and would be preferable for use in the lab. May 15 2020 - 2:23pm
DESCRIPTION
A sulfonylurea receptor 1, Kir6.2 blocker, belonging to the metiglinides drug family.
(GtoPdb)
MOA
Inhibitor
(Chemical Probes.org)
DESCRIPTION
alpha5-selective GABAA inverse agonist
(Tocris Bioactive Compound Library)
DESCRIPTION
Kir6 (KATP) channel blocker
(Tocriscreen Plus)
DESCRIPTION
KATP channel blocker
(Tocriscreen Total)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
0
Compound Sets
37
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
ChEMBL Approved Drugs
ChEMBL Drugs
Chemical Probes.org
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
High-quality chemical probes
LSP-MoA library (Laboratory of Systems Pharmacology)
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
NCATS Inxight Approved Drugs
NIH Clinical Collections (NCC)
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
The Spectrum Collection
Tocris Bioactive Compound Library
Tocriscreen Plus
Tocriscreen Total
Tool Compound Set
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
48
Molecular Weight
452.27
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
2
Rotatable Bonds
10
Ring Count
3
Aromatic Ring Count
2
cLogP
5.22
TPSA
78.87
Fraction CSP3
0.48
Chiral centers
1.0
Largest ring
6.0
QED
0.52
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Ion Channels
Target
Sulfonylurea receptor 1
Potassium Channel
PPAR??
ABCC8, KCNJ11, PPARG
KATP channel blocker
ABCC8, KCNJ11
Pathway
Membrane Transporter/Ion Channel
Metabolism
DNA Damage/DNA Repair
Primary Target
Inward Rectifier Potassium (Kir) Channels
MOA
Blocker
Insulin Secretagogues
insulin secretagogue
Member status
member
Indication
diabetes mellitus
Target subclass
Potassium channel
Potassium channel, Potassium channel
Target class
Ion channel
Ion Channel, Ion Channel
Orthogonal probe
Glyburide
Therapeutic Class
Hypoglycemic Agents
Source data
