Lesogaberan - CAS:344413-67-8

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Lesogaberan (Synonyms:AZD-3355)

目录号 : KM4815 CAS No. : 344413-67-8

Data Sheet 产品使用指南

Lesogaberan (AZD-3355) 是一种有效的选择性 GABA_B 受体激动剂，对人重组 GABA_B 受体的 EC₅₀ 为 8.6 nM。通过脑膜中 [³H]GABA 结合位移测量，Lesogaberan 对大鼠 GABA_B 和 GABA_A 受体的亲和力 (K_is)：分别为 5.1 nM 和 1.4 μM。Lesogaberan 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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10mg		In-stock
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50mg		In-stock

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生物活性

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

体外研究

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

Cell Proliferation Assay

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

Lesogaberan (AZD3355) potently stimulates recombinant human GABA_B 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) protects human islet β-cells from apoptosis in islet grafts in mice.
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.

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

分子式

C₃H₈FNO₂P

分子量

141.08

CAS号

344413-67-8

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.

临床试验

Data Sheet

产品使用指南

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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