2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. Lesogaberan napadisylate

Lesogaberan napadisylate  (Synonyms: AZD-3355 napadisylate)

目录号: HY-10061A
产品使用指南

摩尔计算器

Lesogaberan (AZD-3355) napadisylate 是一种有效的选择性 GABAB 受体激动剂，对人重组 GABAB 受体的 EC50 为 8.6 nM。通过脑膜中 [3H]GABA 结合位移测量，Lesogaberan napadisylate 对大鼠 GABAB 和 GABAA 受体的亲和力 (Kis)：分别为 5.1 nM 和 1.4 μM。Lesogaberan napadisylate 通过外周作用模式抑制短暂的食管下括约肌松弛。

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Lesogaberan napadisylate Chemical Structure

Lesogaberan napadisylate Chemical Structure

CAS No. : 477956-38-0

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Lesogaberan napadisylate 的其他形式现货产品:

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Lesogaberan napadisylate 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action[1].

IC50 & Target

Ki: 5.1±1.2 nM (rat GABAB), 1.4±0.3 μM (rat GABAA)[1]
EC50: 8.6±0.77 nM (human GABAB receptor)[1]
体外研究
(In Vitro)

Lesogaberan (3-30 nM) enhances human islet cell proliferation in vitro[2].

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

Lesogaberan napadisylate 相关抗体:

Cell Proliferation Assay[2]

Cell Line: Human islet cells
Concentration: 3, 10, and 30 nM
Incubation Time: 4 days
Result: Had a small but nonsignificant promitotic effect at 3 nM, while treatment at higher dosages (10 and 30 nM) led to a 2-3-fold increase in proliferation relative to that of islets cultured in medium alone.
体内研究
(In Vivo)

Lesogaberan (AZD3355) potently stimulates recombinant human GABAB receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs, with a biphasic dose-response curve[1].
Oral Lesogaberan (0.08 mg/mL; 48 hours) protects human islet β-cells from apoptosis in islet grafts in mice[2].
Lesogaberan (7 μmol/kg) shows high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats[1].

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

Animal Model: Diabetic NOD/scid mice were implanted with human islets[2]
Dosage: 0.08 mg/mL
Administration: Oral feeding; 48 hours
Result: Significantly reduced the percentages of apoptotic islet cells and increased the frequency of insulin+ β-cells in human islet grafts.
Animal Model: Female Sprague Dawley rats[1]
Dosage: 7 μmol/kg (Pharmacokinetic Analysis)
Administration: Oral
Result: High oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance. Plasma protein binding was 1% in rat and human plasma.
Clinical Trial
分子量

349.31

Formula

C13H17FNO5PS
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Lesogaberan napadisylate 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

Lesogaberan477956-38-0AZD-3355AZD3355AZD 3355GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorIsletCellSurvivalGastroesophagealrefluxdiseaseGERDdiabeteGABABInhibitorinhibitorinhibit

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