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(E)-GABAB receptor antagonist 1

(E)-GABAB receptor antagonist 1

Item no.	HY-129636-100mg
Manufacturer	MedChem Express
CASRN	1611483-29-4
Amount	100 mg
Quantity options	100 mg 1 ea 1 mg
Category	Reagents & Chemicals Biochemicals
Type	Chemicals
Specific against	other
Purity	95.26
Citations	[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.<br/>[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.
Smiles	O=C(C(/C=C/C1=CC(C(C)(C)C)=C(C(C(C)(C)C)=C1)O)=O)O
ECLASS 10.1	32160000
ECLASS 11.0	32160000
UNSPSC	12000000
Available
Product Description	CLH304a (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 receptors[1][2].
StorageTemperature	-20°C, 3 years (Powder)
Shipping	Blue Ice
Manufacturers Applications	Neuroscience-Neuromodulation
MolecularWeight	304.38
Clinical Information	No Development Reported
Manufacturers Research Area	Neurological Disease
Solubility	10 mM in DMSO
Target	ERK; GABA Receptor
Manufacturers Target	ERK; GABA Receptor
Manufacturers Pathway	MAPK/ERK Pathway; Membrane Transporter/Ion Channel; Neuronal Signaling; Stem Cell/Wnt
Manufacturers Product type	Reference compound

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