(E)-GABAB receptor antagonist 1

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CAS:1611483-29-4
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(E)-GABAB receptor antagonist 1 Basic information
Product Name:(E)-GABAB receptor antagonist 1
Synonyms:(E)-GABAB receptor antagonist 1;3-Butenoic acid, 4-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-oxo-, (3E)-;(E) GABAB receptor antagonist 1,(E)GABAB receptor antagonist 1;(E)-GABAB receptor antagonist 1, 10 mM in DMSO
CAS:1611483-29-4
MF:C18H24O4
MW:304.38
EINECS:
Product Categories:
Mol File:1611483-29-4.mol
(E)-GABAB receptor antagonist 1 Structure
(E)-GABAB receptor antagonist 1 Chemical Properties
Boiling point 404.3±37.0 °C(Predicted)
density 1.125±0.06 g/cm3(Predicted)
form Solid
pka2.05±0.54(Predicted)
color Light yellow to yellow
Safety Information
MSDS Information
(E)-GABAB receptor antagonist 1 Usage And Synthesis
UsesCLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor[1][2].
References[1] Chen LH, et al. Discovery of a Negative Allosteric Modulator of GABAB Receptors. ACS Med Chem Lett. 2014 May 27;5(7):742-7. DOI:10.1021/ml500162z
[2] Bing Sun, et al. A negative allosteric modulator modulates GABAB-receptor signalling through GB2 subunits. Biochem J. 2016 Mar 15;473(6):779-87. DOI:10.1042/BJ20150979
(E)-GABAB receptor antagonist 1 Preparation Products And Raw materials
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