General
Preferred name
SARPOGRELATE
Synonyms
Sarpogrelate hydrochloride ()
MCI-9042 ()
sarpogrelate hydrochloride, KunWha Pharmaceutical ()
Sarpogrelate (hydrochloride) ()
LS-187118 ()
SARPOGRELATE HYROCHLORIDE ()
Sarpogrelato ()
Sarpogrelate ()
Sarpogrelate-d3 (hydrochloride) ()
P&D ID
PD014349
CAS
135159-51-2
125926-17-2
2934185-00-7
Tags
available
drug
Drug indication
Peripheral arterial disease
Diabetic complication
Drug Status
approved
investigational
Max Phase
3.0
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 Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, ¦Á1-, ¦Á2- and ¦Â-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].
PRICE 62
DESCRIPTION Sarpogrelate is a 5-HT2A/ 5-HT2B receptor antagonist which blocks serotonin-induced platelet aggregation. (GtoPdb)
DESCRIPTION Potent and selective H3 inverse agonist (Tocris Bioactive Compound Library)
DESCRIPTION Selective 5-HT2A antagonist (Tocriscreen Plus)
DESCRIPTION Sarpogrelate hydrochloride (MCI-9042) , a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. Target: 5-HT2 Recepter Sarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate hydrochloride was shown to have the same affinity as ritanserin for 5-HT2A receptors, with a Ki value of 8.39 nM. Sarpogrelate hydrochloride lacked prominent 5-HT1-like, 5-HT3, beta, H1, H2 and M3 antagonist activity and weakly blocked alpha 1-adrenoceptors (pKB = 6.30). (S)-M-1 showed weak affinity for 5-HT1-like receptors (pKB = 6.30), alpha 1- (pKB = 6.80) and beta- (pKB = 6.54) adrenoceptors, while (R)-M-1 was a weak antagonist at histamine H1 receptors (pKB = 6.49). After 12 weeks of sarpogrelate administration, FBF and LBF responses during RH showed significant increases from 13.2 +/- 1.7 to 18.1 +/- 2.2 mL/min per 100 mL tissue (P < 0.01) and from 8.2 +/- 0.9 to 14.2 +/- 2.1 mL/min per 100 mL tissue (P < 0.05), respectively. Sarpogrelate hydrochloride -induced augmentation of FBF and LBF responses to RH was maintained at 24 weeks. Long-term oral administration of sarpogrelate improves vascular function in patients with PAD. (TargetMol Bioactive Compound Library)
DESCRIPTION Sarpogrelate is a drug under the development of Mitsubishi Chemical as 5HT2A and 5-HT2B receptor. antagonists. It is used as an antiplatelet agent and has been applicated for the treatment of many diseases including coronary artery disease, diabetes mellitus, Buerger's disease, angina pectoris, Raynaud's disease, and atherosclerosis. (BOC Sciences Bioactive Compounds)
Cell lines
0
Organisms
1
Compound Sets
17
BOC Sciences Bioactive Compounds
sarpogrelate-cas-125926-17-2-item-56537
Cayman Chemical Bioactives
24194
33472
ChEMBL Drugs
CHEMBL52939
DrugBank
DB12163
DrugCentral
2423
DrugCentral Approved Drugs
2423
DrugMAP
DMGLP6S
DrugMAP Approved Drugs
DMGLP6S
DrugMatrix
Guide to Pharmacology
210
MedChem Express Bioactive Compound Library
HY-10564
NPC Screening Collection
ReFrame library
Selleckchem Bioactive Compound Library
sarpogrelate-hydrochloride
TargetMol Bioactive Compound Library
T4978
Tocris Bioactive Compound Library
3739
Tocriscreen Plus
3739
External IDs
45
Properties
(calculated by RDKit )
Molecular Weight
429.22
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
1
Rotatable Bonds
13
Ring Count
2
Aromatic Ring Count
2
cLogP
3.2
TPSA
85.3
Fraction CSP3
0.42
Chiral centers
1.0
Largest ring
6.0
QED
0.49
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
7-TM Receptors
Target
5-HT Receptor
5-HT2
5-HT2A
Primary Target
5-HT2A Receptors
MOA
Antagonist
Therapeutic Class
Hypoglycemic Agents
Pathway
GPCR/G protein
Neuronal Signaling
Neuroscience
Solubility
Soluble in DMSO
Source data