General
Preferred name
treprostinil
Synonyms
LRX-15 ()
Orenitram ()
Remodulin ()
UT-15C ()
Treprostinil Sodium ()
Treprostinil (sodium) ()
Treprostinil (diethanolamine) ()
UT-15 ()
UT-15 (sodium) ()
UT-15, Remodulin, Orenitram, Tyvaso, Trevyent ()
Treprostinil diethanolamine ()
TREPROSTINIL DIOLAMINE ()
Treprostinil (diethanolamine salt) ()
Treprostinil diolamin ()
15AU81 ()
L606 ()
15-AU-81 ()
Tresprostinil ()
Tyvaso dpi ()
LRX -15 ()
Treprostinilo ()
L-606 ()
Rumodolin ()
Uniprost ()
Tyvaso ()
Trepulmix ()
Treprostinil sodium salt ()
Yutrepia ()
P&D ID
PD010219
CAS
81846-19-7
289480-64-4
830354-48-8
Tags
available
drug
Approved by
FDA
PMDA
EMA
First approval
2013
2002
2020
Drug indication
Pulmonary hypertension
ischemia reperfusion injury
Pulmonary arterial hypertension
systemic scleroderma
Drug Status
approved
investigational
Max Phase
4.0
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 Treprostinil (UT-15C) diethanolamine is a potent EP2, DP1 and IP agonist with Ki values of 3.6, 4.4, 32.1, 212, 826, 2505 and 4680 nM for EP2, DP1, IP, EP1, EP4, EP3 and FP, respectively. Treprostinil (UT-15C) diethanolamine increases upregulation of cAMP toward maintaining homeostasis within the vasculature. Treprostinil (UT-15C) diethanolamine can result in vasodilatation of human pulmonary arteries[1][2][3].
PRICE 410
DESCRIPTION Marketed formulations may contain treprostinil diolamine (PubChem CID 11179459) or treprostinil sodium (PubChem CID 23663413). (GtoPdb)
METABOLISM Substantially metabolized by the liver, but the precise enzymes responsible are unknown. Five metabolites have been described (HU1 through HU5) however, the biological activity and metabolic fate of these are unknown. The chemical structure of HU1 is unknown. The metabolite HU5 is the glucuronide conjugate of treprostinil. The other metabolites are formed by oxidation of the 3-hydroxyoctyl side chain (HU2) and subsequent additional oxidation (HU3) or dehydration (HU4). Study results of in vitro human hepatic cytochrome P450 demonstrates that treprostinil does not inhibit CYP-1A2, 2C9, 2C19, 2D6, 2E1, or 3A. There have been no studies that evaluate the potential of treprostinil to induce these enzymes.
DESCRIPTION Treprostinil (UT-15) is a potent DP1 and EP2 agonist with EC50 values of 0.6¡À0.1 and 6.2¡À1.2 nM, respectively.
PRICE 100
DESCRIPTION Treprostinil (UT-15) sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6¡À0.1 and 6.2¡À1.2 nM, respectively.
PRICE 124
DESCRIPTION Treprostinil Sodium (UT-15) is a potent DP1, IP and EP2 agonist (EC50: 0.6/1.9/6.2 nM).
DESCRIPTION Treprostinil diethanolamine (UT-15C) is a potent agonist of EP2, DP1, and IP, with values of 3.6, 4.4, and 32.1 nM for EP2, DP1, and IP, respectively, and 212, 826, 2505, and 4680 nM for EP1, EP4, EP3, and FPKi, respectively. Treprostinil diethanolamine contributes to the upregulation of cAMP, maintaining vascular homeostasis and causing vasodilation in human pulmonary arteries. (TargetMol Bioactive Compound Library)
DESCRIPTION Potent and selective GPR39 agonist (Tocris Bioactive Compound Library)
DESCRIPTION Treprostinil is a synthetic analogue of prostacyclin, used to treat pulmonary hypertension. It t binds to the prostacyclin receptor. (Enamine Bioactive Compounds)
DESCRIPTION Treprostinil (Orenitram) is a potent DP1, IP and EP2 agonist (EC50: 0.6/1.9/6.2 nM). (TargetMol Bioactive Compound Library)
Compound Sets
27
AdooQ Bioactive Compound Library
A13719
A21046
Cayman Chemical Bioactives
11927
10162
ChEMBL Approved Drugs
CHEMBL2107815
CHEMBL1237119
CHEMBL561157
ChEMBL Drugs
CHEMBL2107815
CHEMBL1237119
CHEMBL561157
Concise Guide to Pharmacology 2017/18
5820
Concise Guide to Pharmacology 2019/20
5820
Concise Guide to Pharmacology 2021/22
5820
Concise Guide to Pharmacology 2023/24
5820
Drug Repurposing Hub
DrugBank
DB00374
DrugBank Approved Drugs
DB00374
DrugCentral
2720
DrugCentral Approved Drugs
2720
DrugMAP
DMTIQF3
DrugMAP Approved Drugs
DMTIQF3
Enamine Bioactive Compounds
EBC-26916
EU-OPENSCREEN Bioactive Compound Library
EOS100648
Guide to Pharmacology
5820
Mcule NIBR MoA Box Subset
MCULE-1786426561
MedChem Express Bioactive Compound Library
HY-B0813
HY-100441
HY-16504
Natural product-based probes and drugs
NCATS Inxight Approved Drugs
RUM6K67ESG
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
treprostinil-sodium
TargetMol Bioactive Compound Library
T63349
T5150
Tocris Bioactive Compound Library
5349
External IDs
74
Properties
(calculated by RDKit )
Molecular Weight
390.24
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
3
Rotatable Bonds
10
Ring Count
3
Aromatic Ring Count
1
cLogP
3.58
TPSA
86.99
Fraction CSP3
0.7
Chiral centers
5.0
Largest ring
6.0
QED
0.53
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
DP1
EP2
IP
Prostaglandin Receptor
P2RY12, PPARD, PTGIR
Primary Target
Prostanoid Receptors
MOA
Agonist
Prostacyclin Analogs
prostanoid receptor agonist
Member status
member
Indication
pulmonary arterial hypertension (PAH)
Biosynthetic Origin
Fatty Acid (Eicosanoid)
Therapeutic Indication
Antihypertensive
Therapeutic Class
Cardiovascular
Antihypertensive Agents
Pathway
GPCR/G protein
Immunology/Inflammation
Source data