Identification | Back Directory | [Name]
PRE-084 | [CAS]
138847-85-5 | [Synonyms]
I-AMB PRE-084 J000280 J-000280 BIMI1803 BIMI-1803 4-MeO-PBP PRE-084HCl ZXAFC000547 ZX-AFC000547 PRE-084 HYDROCHLORIDE PRE-084;PRE 084;PRE084 2-Morpholinoethyl 1-phenylcyclohexanecarboxylate 2-(4-MORPHOLINETHYL)-1-PHENYLCYCLOHEXANECARBOXYLATE HCL 2-(4-morpholino)ethyl-1-phenylcyclohexane-1-carboxylate 2-morpholin-4-ylethyl 1-phenylcyclohexane-1-carboxylate 1-Phenylcyclohexanecarboxylic acid 2-morpholinoethyl ester 2-(4-MORPHOLINETHYL) 1-PHENYLCYCLOHEXANECARBOXYLATE HYDROCHLORIDE Cyclohexanecarboxylicacid, 1-phenyl-, 2-(4-morpholinyl)ethyl ester | [Molecular Formula]
C19H27NO3 | [MDL Number]
MFCD00673883 | [MOL File]
138847-85-5.mol | [Molecular Weight]
317.42 |
Chemical Properties | Back Directory | [Boiling point ]
446.6±40.0 °C(Predicted) | [density ]
1.103±0.06 g/cm3(Predicted) | [storage temp. ]
Store at RT | [solubility ]
H2O: ≤24 mg/mL | [form ]
solid | [pka]
5.99±0.10(Predicted) | [color ]
White | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months. |
Hazard Information | Back Directory | [Description]
PRE084 (138847-85-8) is an agonist of the σ receptor with selectivity for the σ1 subtype?(IC50’s: σ1 = 2.2nM, σ2 = 13091nM).1?PRE-084 has demonstrated neuroprotective/restorative effects in brain injury2,3?and neurodegenerative conditions4-7. | [Definition]
ChEBI:1-phenyl-1-cyclohexanecarboxylic acid 2-(4-morpholinyl)ethyl ester is a member of morpholines. | [Biological Activity]
High affinity, selective σ 1 agonist (K i values are 2.2 and 13091 nM for σ 1 and σ 2 receptors respectively). Selective over PCP receptors (IC 50 > 100000 nM) and several other receptor systems. Produces antiamnesic and antitussive effects in vivo . | [Biochem/physiol Actions]
PRE-084 is a potent and highly selective σ1 opioid receptor agonist. It offers neuroprotection upon embolic stroke. | [storage]
Store at RT | [References]
1) Su?et al.?(1991),?Sigma compounds derived from phencyclidine. Identification of PRE-084, a new selective sigma ligand; J. Pharmacol. Exp. Ther.?259?543
2) Griesmaier?et al.?(2012),?Neuroprotective effects of the sigma-1 receptor ligand PRE-084 against excitotoxic perinatal brain injury in newborn mice; Exp. Neurol.?237?388
3) Dong?et al.?(2016),?Sigma-1 Receptor Modulates Neuroinflammation After Traumatic Brain Injury; Cell Mol. Neurobiol.?36?639
4) Guzman-Lenis?et al.?(2009),?Selective sigma receptor agonist 2-(4-Morpholinethyl) 1-phenylcyclohexanecarboxylate (PRE084) promotes neuroprotection and neurite elongation through protein kinase C (PKC) signaling on motoneurons; Neuroscience?162?31
5) Hyrskyluoto?et al.?(2013),?Sigma-1 receptor agonist PRE084 in protective against mutant huntingtin-induced cell degeneration: involvement of calpastatin and the NF-κB pathway; Cell Death Dis.?4?e646
6) Francardo?et al.?(2014),?Pharmacological stimulation of sigma-1 receptors has neurorestorative effects in experimental parkinsonism; Brain?137(Pt7)?1998
7) Mancuso?et al.?(2012),?Sigma-1R agonist improves motor function and motoneuron survival in ALS mice; Neurotherapeutics?9?814 |
|
Company Name: |
DeboraLabs
|
Tel: |
+44 2032 895 122 |
Website: |
www.deboralabs.com |
Company Name: |
Sigma-Aldrich
|
Tel: |
021-61415566 800-8193336 |
Website: |
https://www.sigmaaldrich.cn |
|