1611483-29-4
Chemical Structure
CLH304a
Synonym(s): (E)-GABAB receptor antagonist 1
- CAS No.: 1611483-29-4
- Formula:C18H24O4
- Molecular Weight:304.38
IUPAC Name: (E)-4-(3,5-di-tert-butyl-4-hydroxyphenyl)-2-oxobut-3-enoic acid
InChIKey: XIQDGAUDNMVMCD-BQYQJAHWSA-N
SMILES: O=C(C(/C=C/C1=CC(C(C)(C)C)=C(C(C(C)(C)C)=C1)O)=O)O
Biological Activity: 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 receptor[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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CLH304a | 99.64% | 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 receptor. | ||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
Keywords
