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Lesogaberan

(Synonyms: P-[(2R)-3-氨基-2-氟丙基]磷酸,AZD-3355) 目录号 : GC61624

Lesogaberan(AZD-3355)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8.6nM。对大鼠脑GABAB和GABAA受体的结合亲和力(Ki)分别为5.1nM和1.4μM。

规格 价格 库存 购买数量
5 mg
¥3,600.00
现货
10 mg
¥6,120.00
现货
25 mg
¥12,150.00
现货
50 mg
¥20,700.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABAB and GABAA receptors, respectively[1].

Lesogaberan (3-30 nM) enhances human islet cell proliferation in vitro[2]. Cell Proliferation Assay[2] Cell Line: Human islet cells

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]. Animal Model: Diabetic NOD/scid mice were implanted with human islets[2]

[1]. Lehmann A, et al. (R)-(3-amino-2-fluoropropyl) phosphinic acid (AZD3355), a novel GABAB receptor agonist, inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action. J Pharmacol Exp Ther. 2009 Nov;331(2):504-12. [2]. Tian J, et al. Repurposing Lesogaberan to Promote Human Islet Cell Survival and β-Cell Replication. J Diabetes Res. 2017;2017:6403539.

Chemical Properties

Cas No. 344413-67-8 SDF
别名 P-[(2R)-3-氨基-2-氟丙基]磷酸,AZD-3355
化学名 N/A
Canonical SMILES O=P(C[C@H](F)CN)O
分子式 C3H9FNO2P 分子量 141.08
溶解度 N/A 储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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