2. Membrane Transporter/Ion Channel Neuronal Signaling Stem Cell/Wnt MAPK/ERK Pathway
  3. GABA Receptor ERK
  4. CLH304a

CLH304a  (Synonyms: (E)-GABAB receptor antagonist 1)

Cat. No.: HY-129636 Purity: 95.26%
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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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CLH304a Chemical Structure

CLH304a Chemical Structure

CAS No. : 1611483-29-4

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Based on 1 publication(s) in Google Scholar

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ERK ERK1 ERK2 ERK5 ERK8

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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].

In Vitro

(E)-GABAB receptor antagonist 1 (compound 14) decreases agonist GABA-induced maximal effect of IP3 production in HEK293 cells overexpressing GABAB receptors and Gqi9 proteins without changing the EC50[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CLH304a Related Antibodies
Molecular Weight

304.38

Formula

C18H24O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (164.27 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2854 mL 16.4268 mL 32.8537 mL
5 mM 0.6571 mL 3.2854 mL 6.5707 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2854 mL 16.4268 mL 32.8537 mL 82.1342 mL
5 mM 0.6571 mL 3.2854 mL 6.5707 mL 16.4268 mL
10 mM 0.3285 mL 1.6427 mL 3.2854 mL 8.2134 mL
15 mM 0.2190 mL 1.0951 mL 2.1902 mL 5.4756 mL
20 mM 0.1643 mL 0.8213 mL 1.6427 mL 4.1067 mL
25 mM 0.1314 mL 0.6571 mL 1.3141 mL 3.2854 mL
30 mM 0.1095 mL 0.5476 mL 1.0951 mL 2.7378 mL
40 mM 0.0821 mL 0.4107 mL 0.8213 mL 2.0534 mL
50 mM 0.0657 mL 0.3285 mL 0.6571 mL 1.6427 mL
60 mM 0.0548 mL 0.2738 mL 0.5476 mL 1.3689 mL
80 mM 0.0411 mL 0.2053 mL 0.4107 mL 1.0267 mL
100 mM 0.0329 mL 0.1643 mL 0.3285 mL 0.8213 mL
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CLH304a Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CLH304a1611483-29-4(E)-GABAB receptor antagonist 1GABA ReceptorERKGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorExtracellular signal regulated kinasesGABABnegative allosteric modulatorNAMIP3mGluR1mGluR2mGluR5GB2ERK1/2Inhibitorinhibitorinhibit

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