CLH304a

• 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 receptor[1][2].

• 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

• CAS Number:

  [1611483-29-4]