SML3300
TB21007
≥98% (HPLC)
别名:
3-(2-Hydroxyethylthio)-6,6-dimethyl-1-(thiazol-2-yl)-6,7-dihydrobenzo[c]thiophen-4(5H)-one, 6,6-Dimethyl-3-(2-hydroxyethyl)thio-1-(thiazol-2-yl)-6,7-dihydro-2-benzothiophen-4(5H)-one, 6,7-Dihydro-3-[(2-hydroxyethyl)thio]-6,6-dimethyl-1-(2-thiazolyl)benzo[c]thiophen-4(5H)-one, TB 21007, TB-21007
InChI
1S/C15H17NO2S3/c1-15(2)7-9-11(10(18)8-15)14(20-6-4-17)21-12(9)13-16-3-5-19-13/h3,5,17H,4,6-8H2,1-2H3
InChI key
QILRYFCEXLFIDS-UHFFFAOYSA-N
SMILES string
O=C1C2=C(SCCO)SC(C3=NC=CS3)=C2CC(C1)(C)C
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Gamma-aminobutyric acid type A receptor GABA(A) alpha 5 (α5) subtype-selective inverse agonist/negative allosteric modulator (NAM) in vitro and in vivo.
TB21007 is a gamma-aminobutyric acid type A receptor (GABAA) alpha 5 (α5) subtype-selective (αβ3γ2 Ki in nM = 1.6/α5, 20/α1, 16/α2, 20/α3) negative allosteric modulator (NAM)/inverse agonist (% inhibition at 100 nM = 51/α5, 21/α1, 1/α2, 3/α3, using L(tk-) fibroblast expressing β3γ2 with respective α subunit). TB21007 enhances cognitive performance in a hippocampal-dependent memory task in vivo (0.3 mg/kg i.p. in rats; delayed ‘matching-to-place′ Morris water maze test) without the convulsant or proconvulsant activity (3 mg/kg i.p. in mice) observed with nonselective inverse agonists.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Ming Teng Koh et al.
Neurobiology of aging, 91, 1-4 (2020-04-03)
Numerous aging studies have identified a shift in the excitatory/inhibitory (E/I) balance with heightened hippocampal neural activity associated with age-related memory impairment across species, including rats, monkeys, and humans. Neurobiological investigations directed at the hippocampal formation have demonstrated that unimpaired
Yarim E De la Luz-Cuellar et al.
European journal of pharmacology, 858, 172443-172443 (2019-06-11)
The role of spinal α5 subunit-containing GABAA (α5-GABAA) receptors in chronic pain is controversial. The purpose of this study was to investigate the participation of spinal α5-GABAA receptors in the reserpine-induced pain model. Reserpine administration induced tactile allodynia and muscle
Mark S Chambers et al.
Journal of medicinal chemistry, 46(11), 2227-2240 (2003-05-16)
In pursuit of a GABA(A) alpha5-subtype-selective inverse agonist to enhance cognition, a series of 6,7-dihydro-2-benzothiophen-4(5H)-ones has been identified as a novel class of GABA(A) receptor ligands. These thiophenes have higher binding affinity for the GABA(A) alpha5 receptor subtype compared to
K McEown et al.
Neuroscience, 252, 169-177 (2013-08-22)
Temporary neuronal inactivation of the ventral hippocampus with the GABAA agonist muscimol suppresses unconditioned fear behavior (anxiety) but inactivation of the dorsal hippocampus does not. On the other hand, inactivating the dorsal hippocampus disrupts fear memory, while inactivating the ventral
Ming Teng Koh et al.
Neuropharmacology, 64, 145-152 (2012-06-27)
A condition of excess activity in the hippocampal formation is observed in the aging brain and in conditions that confer additional risk during aging for Alzheimer's disease. Compounds that act as positive allosteric modulators at GABA(A) α5 receptors might be
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