(E/Z)-CLH304a
(E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors.
For research use only. We do not sell to patients.
- CAS No.: 797-17-1
- Formula: C18H24O4
- Molecular Weight:304.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
37.9 μM
Compound: 14
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Negative allosteric modulation of recombinant HA-tagged GB1 subunit/Flag-tagged GB2 subunit receptor (unknown origin) expressed in HEK293 cells co-expressing Gqi9 G-protein assessed as inhibition of GABA-induced IP production by liquid scintillation count
Negative allosteric modulation of recombinant HA-tagged GB1 subunit/Flag-tagged GB2 subunit receptor (unknown origin) expressed in HEK293 cells co-expressing Gqi9 G-protein assessed as inhibition of GABA-induced IP production by liquid scintillation count
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[PMID: 25050158] |
| HEK293 | IC50 |
37.9 μM
Compound: 22
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Negative allosteric modulator activity at GABA-B receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of GABA-induced inositol phosphate production
Negative allosteric modulator activity at GABA-B receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of GABA-induced inositol phosphate production
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[PMID: 25856547] |
Chemical Information
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CAS No. 797-17-1
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Molecular Weight 304.38
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Formula C18H24O4
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SMILES
O=C(O)C(/C=C/C1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1)=O
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Synonyms
GABAB receptor antagonist 1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
DMSO : ≥ 200 mg/mL (657.07 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (16.43 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
[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]
Complete Stock Solution Preparation Table
| 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 |
(E/Z)-CLH304a Related Classifications
HY-129636A Related Classifications
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