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Lesogaberan is an effective and selective GABAB receptor agonist (EC50: 8.6 nM for human recombinant GABAB receptors). For rat brain GABAB and GABAA receptors, the binding affinity (Kis) is 5.1 nM and 1.4 μM, respectively.
别名 AZD-3355
Lesogaberan is an effective and selective GABAB receptor agonist (EC50: 8.6 nM for human recombinant GABAB receptors). For rat brain GABAB and GABAA receptors, the binding affinity (Kis) is 5.1 nM and 1.4 μM, respectively.

| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 25 mg | ¥ 10,600 | 6-8周 | |
| 50 mg | ¥ 13,800 | 6-8周 | |
| 100 mg | ¥ 17,500 | 6-8周 |
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| 产品描述 | Lesogaberan is an effective and selective GABAB receptor agonist (EC50: 8.6 nM for human recombinant GABAB receptors). For rat brain GABAB and GABAA receptors, the binding affinity (Kis) is 5.1 nM and 1.4 μM, respectively. |
| 靶点活性 | GABAA (rat):1.4±0.3 μM(ki), GABAB (rat):(ki)5.1±1.2 nM, GABAB receptor (human):(EC50)8.6±0.77 nM |
| 体外活性 | Lesogaberan (3-30 nM) increases a human islet cell proliferation in vitro[2]. |
| 体内活性 | Lesogaberan effectively stimulates recombinant human GABAB receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs, with a biphasic dose-response curve[1]. Lesogaberan (7 μmol/kg) displays high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats[1]. Lesogaberan (0.08?mg/mL; 48 hours; p.o.) treatment, protects human islet β-cells from apoptosis in islet grafts in mice[2]. |
| 别名 | AZD-3355 |
| 分子量 | 141.08 |
| 分子式 | C3H9FNO2P |
| CAS No. | 344413-67-8 |
| Smiles | [C@H](CP(=O)O)(CN)F |
| 密度 | 1.31g/cm3 |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. 实际储存温度请以COA为准 |
对于不同动物的给药剂量换算,您也可以参考 更多