Product Details
| Product Name:
E2730 |
CAS No.:
1520073-91-9 |
| Purity:
98.54% |
Supply Ability:
10g |
| Release date:
2025/11/10 |
Product Introduction
Bioactivity
| Name | E2730 |
| Description | E2730 is an orally active, selective, and non-competitive GABA transporter 1 (GAT1) inhibitor with antiepileptic activity, used in neurological disease research. |
| In vitro | The 50% inhibition concentration (IC50) of E2730 was 1.1 μM for hGAT1, >1000 μM for hGAT2, >1000 μM for hGAT3, and 890 μM for hBGT-1.
E2730 (0.0128-1000 μM) inhibited GAT1 in a non-competitive manner, and its inhibition was positively correlated with GABA levels in vitro. E2730 also increases extracellular GABA concentration under overactivation conditions. [1] |
| In vivo | E2730 (20-400mg/kg orally) showed antiepileptic effects in corneal ignition, 6 Hz-44 mA psychomotor seizures, amygdala ignition, Fragile X syndrome, and Dravet syndrome models.
The 50% effective dose (ED50) of E2730 was 7.9 mg/kg in cornea-ignited mice and the 50% toxic dose (TD50) was 350 mg/kg in accelerated rotation tests. The E2730 has a protection index (i.e. the ratio of TD50 to ED50) of 44.3. [1] |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Keywords | GABAReceptor | GABA Receptor |
| Inhibitors Related | Valproic acid sodium salt | p-Hydroxybenzaldehyde | Urethane | Baicalin | Penicillin G sodium salt | Valproic Acid | Halothane | Chlorothymol | Piperazine citrate | (-)-α-Pinene | Dihydromyricetin | Methionine |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Neurotransmitter Receptor Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library |
Company Profile Introduction
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries， 10000+ Noval Small Molecucles，16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States