General
Preferred name
E-3174
Synonyms
Losartan (D4 Carboxylic Acid) ()
E-3174 D4 ()
EXP-3174 D4 ()
E 3174 ()
EXP3174 ()
EXP-3174 ()
EXP 3174 ()
Carboxylosartan ()
Losartan Carboxylic Acid ()
Losartan Carboxylic Acid (EXP-3174) ()
CARBOXYLIC ACID METABOLITE ()
P&D ID
PD018082
CAS
124750-92-1
Tags
available
drug candidate
Drug indication
Discovery agent
Probe control
Probe control not defined
Orthogonal probes
0
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)
DESCRIPTION
Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure[1][2][3][4].
PRICE
35
DESCRIPTION
Potent and selective V1B receptor antagonist; orally bioavailable
(Tocris Bioactive Compound Library)
DESCRIPTION
Losartan Carboxylic Acid (E-3174), a potent AT1 antagonist (Kis: 0.57 nM, rat; 0.67 nM, human), produces a depressor response and vasodilatation. As a metabolite of losartan, it is more potent than losartan in blocking angiotensin II-induced responses in vascular smooth muscle cells.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
1
Compound Sets
12
Cayman Chemical Bioactives
Concise Guide to Pharmacology 2017/18
Drug Repurposing Hub
DrugMAP
Guide to Pharmacology
MedChem Express Bioactive Compound Library
Other bioactive compounds
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
39
Molecular Weight
436.14
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
2
Rotatable Bonds
8
Ring Count
4
Aromatic Ring Count
4
cLogP
4.47
TPSA
109.58
Fraction CSP3
0.23
Chiral centers
0.0
Largest ring
6.0
QED
0.42
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Angiotensin Receptor
AT1 receptor
AGTR1
Drug Metabolite
Pathway
GPCR/G protein
Metabolic Enzyme/Protease
Endocrinology/Hormones
Primary Target
Angiotensin AT1 Receptors
MOA
Antagonist
angiotensin antagonist
Source data
