General
Preferred name
TALTIRELIN
Synonyms
Ceredist ()
taltirelin hydrate ODT ()
Taltirelin (acetate) ()
TA-0910 ()
TA-0910 (acetate) ()
Taltirelina ()
Taltireline ()
Taltirelin acetate ()
P&D ID
PD012122
CAS
103300-74-9
1549593-23-8
Tags
available
drug candidate
Drug Status
investigational
Max Phase
2.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca2+ concentration (Ca2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue[1][2][3].
DESCRIPTION
Taltirelin acetate (TA-0910) is an acetate form of Taltirelin (TA-0910). Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca2+ concentration (Ca2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue[1][2][3].
PRICE
120
DESCRIPTION
Taltirelin acetate (TA-0910 acetate) is a superagonist of the thyrotropin-releasing hormone receptor (TRH-R), with an IC50 of 910 nM and an EC50 of 36 nM for stimulating an increase in cytosolic Ca2+ concentration (Ca2+ release).
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
9
AdooQ Bioactive Compound Library
ChEMBL Drugs
Drug Repurposing Hub
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
Natural product-based probes and drugs
NPC Screening Collection
ReFrame library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
35
Molecular Weight
405.18
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
4
Rotatable Bonds
6
Ring Count
3
Aromatic Ring Count
1
cLogP
-2.15
TPSA
170.59
Fraction CSP3
0.53
Chiral centers
3.0
Largest ring
6.0
QED
0.42
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Indication
spinocerebellar ataxia
Target
TRHR
Apoptosis
Thyroid hormone receptor
MOA
thyrotropin releasing hormone receptor agonist
Biosynthetic Origin
Peptide (Ribosomal)
Therapeutic Indication
CNS Stimulant
Therapeutic Class
Hormone Therapy
Pathway
Vitamin D Related/Nuclear Receptor
Source data

