产品
编 号：F756978
分子式：C3H10ClFNO2P
分子量：177.54
分子式：C3H10ClFNO2P
分子量：177.54
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
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询价
结构图
CAS No: 2925644-17-1
产品详情
生物活性：
Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride 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 hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
体内研究：
Lesogaberan hydrochloride potently stimulates recombinant human GABAB receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs, with a biphasic dose-response curve.Oral Lesogaberan (0.08?mg/mL; 48 hours) hydrochloride protects human islet β-cells from apoptosis in islet grafts in mice. Lesogaberan (7 μmol/kg) hydrochloride shows high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats.Animal Model:Diabetic NOD/scid mice were implanted with human islets
Dosage:0.08?mg/mL
Administration: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
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.
体外研究：
Lesogaberan hydrochloride (3-30 nM) enhances human islet cell proliferation in vitro.
Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride 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 hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
体内研究：
Lesogaberan hydrochloride potently stimulates recombinant human GABAB receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs, with a biphasic dose-response curve.Oral Lesogaberan (0.08?mg/mL; 48 hours) hydrochloride protects human islet β-cells from apoptosis in islet grafts in mice. Lesogaberan (7 μmol/kg) hydrochloride shows high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats.Animal Model:Diabetic NOD/scid mice were implanted with human islets
Dosage:0.08?mg/mL
Administration: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
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.
体外研究：
Lesogaberan hydrochloride (3-30 nM) enhances human islet cell proliferation in vitro.
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