General
Preferred name
Olodanrigan
Synonyms
EMA401 sodium ()
PD-126055 sodium ()
PD126055 sodium ()
EMA-401 sodium ()
PD-126055 ()
EMA401 ()
EMA-401 ()
(S)-EMA400 ()
PD-126055, (S) PD-126055 ()
Olodanrigan (EMA401) ()
Olodanrigan sodium ()
Ema401 ()
P&D ID
PD046899
CAS
1316755-16-4
1316755-17-5
Tags
available
drug candidate
Drug indication
Peripheral neuropathy
Diabetic neuropathy
Postherpetic neuralgia
Drug Status
investigational
Max Phase
2.0
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 Olodanrigan (EMA401) is reported as a selective antagonist of the angiotensin type II receptor (AT2R) . The compound is being assessed as a novel therapy for neuropathic pain .
Note that PubChem CID 23683656 refers to the potassium salt and that the sodium salt was used in . (GtoPdb)
DESCRIPTION Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. It is under development as a neuropathic pain therapeutic agent. Olodanrigan (EMA401) analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons[1][2][3][4].
PRICE 68
PRICE 1243
DESCRIPTION EMA401 is an orally bioavailable, potent and highly selective antagonist of the angiotensin II type 2 receptor (AT2; IC50s = 39.5 and 408,000 nM for rat recombinant AT2 and AT1, respectively). It inhibits capsaicin-induced calcium influx in cultured human dorsal root ganglion (hDRG) neurons (IC50 = 10 nM) and reduces neurite density and length in rat DRG neuronal cultures. (BOC Sciences Bioactive Compounds)
DESCRIPTION Olodanrigan (EMA401), a highly selective AT2R antagonist, inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons. EMA401 blocks p38, p42/p44 mitogen-activated protein kinase (MAPK) activation, neurite outgrowth in adult rat DRG neurons, and sensitization of adult rat and human DRG neurons induced by AngII. It inhibits capsaicin responses in cultured hDRG neurons. (TargetMol Bioactive Compound Library)
DESCRIPTION Olodanrigan sodium (EMA-401 sodium) is an orally active and selective angiotensin II type 2 receptor (AT2R) antagonist, which can be used in research on neurological diseases. (TargetMol Bioactive Compound Library)
Compound Sets
18
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
MedChem Express Bioactive Compound Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
External IDs
26
Properties
(calculated by RDKit )
Molecular Weight
507.2
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
1
Rotatable Bonds
8
Ring Count
5
Aromatic Ring Count
4
cLogP
5.44
TPSA
76.07
Fraction CSP3
0.19
Chiral centers
1.0
Largest ring
6.0
QED
0.34
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
AT2 receptor
angiotensin II receptor
Angiotensin Receptor
MOA
RAAS
angiotensin antagonist
Pathway
GPCR/G protein
Endocrinology/Hormones
Recommended Cell Concentration
100 nM
Source data