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CLH304a

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].

Product Specifications

CAS Number

[1611483-29-4]

Product Name Alternative

(E) -GABAB receptor antagonist 1

UNSPSC

12352005

Target

ERK; GABA Receptor

Type

Reference compound

Related Pathways

MAPK/ERK Pathway; Membrane Transporter/Ion Channel; Neuronal Signaling; Stem Cell/Wnt

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/clh304a.html

Purity

99.64

Solubility

DMSO : ≥ 100 mg/mL

Smiles

O=C(C(/C=C/C1=CC(C(C)(C)C)=C(C(C(C)(C)C)=C1)O)=O)O

Molecular Formula

C18H24O4

Molecular Weight

304.38

References & 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.|[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.

Shipping Conditions

Blue Ice

Storage Conditions

-20°C, 3 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Available Sizes

Curated Selection

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