General
Preferred name
P1075
Synonyms
U-83757 ()
P-1075 ()
GUANIDINE ()
1-cyano-2-(2-methylbutan-2-yl)-3-pyridin-3-ylguanidine ()
P1075 ()
P&D ID
PD002981
CAS
60559-98-0
Tags
available
drug candidate
Drug indication
Hypertension
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation[1]. P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts[2].
PRICE 122
DESCRIPTION P 1075 is a Kir6 (KATP) channel opener (EC50 for relaxation of rat aorta = 7.5 nM) by causing relaxation of various isolated animal and human blood vessels. (BOC Sciences Bioactive Compounds)
DESCRIPTION P-1075 is a potent sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6) activator (EC50 = 45 nM). P-1075 opens opens mitoKATP channels and may be cardioprotective. (TargetMol Bioactive Compound Library)
DESCRIPTION alpha7 neuronal nAChR antagonist (Tocris Bioactive Compound Library)
Cell lines
0
Organisms
1
Compound Sets
12
BOC Sciences Bioactive Compounds
p1075-cas-60559-98-0-item-77026
Cayman Chemical Bioactives
21849
CZ-OPENSCREEN Bioactive Library
DrugMAP
DM02ANM
DrugMatrix
EUbOPEN Chemogenomics Library
EUB0001926
Ki Database
P1075
MedChem Express Bioactive Compound Library
HY-108573
NIH Clinical Collections (NCC)
ReFrame library
TargetMol Bioactive Compound Library
T16420
Tocris Bioactive Compound Library
1355
External IDs
30
Properties
(calculated by RDKit )
Molecular Weight
231.15
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
2
Rotatable Bonds
3
Ring Count
1
Aromatic Ring Count
1
cLogP
2.11
TPSA
73.1
Fraction CSP3
0.42
Chiral centers
0.0
Largest ring
6.0
QED
0.47
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
SUR2-KIR6
Potassium Channel
Primary Target
Inward Rectifier Potassium (Kir) Channels
MOA
Activator
Pathway
Membrane Transporter/Ion Channel
Recommended Cell Concentration
1 uM
Source data