中文名称: Lesogaberan
英文名称: Lesogaberan
CAS No: 344413-67-8
分子式: C3H9FNO2P
分子量: 141.08
L10500 Lesogaberan ≥98% (psaitong)
包装规格:
5mg in glass bottle
产品描述:

基本信息

产品编号:

L10500

产品名称:

Lesogaberan

CAS:

344413-67-8

 

储存条件

粉末

-20℃

四年

分子式:

C3H9FNO2P

溶于液体

-80℃

二年

分子量:

141.08

 

 

化学名: 

[(2R)-3-amino-2-fluoropropyl]-hydroxy-oxophosphanium

Solubility (25°C):

 

体外:

 

DMSO

 

Ethanol

 

Water

 

体内(现配现用):

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。

 

生物活性

产品描述

一种有效的选择性GABAB受体激动剂

靶点

Ki:5.1±1.2nM (rat GABAB),1.4±0.3μM (rat GABAA)

EC50:8.6±0.77nM (human GABAB receptor)

体外研究

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

Cell Proliferation Assay

Cell Line:

Human islet cells

Concentration:

3,10,and 30nM

Incubation Time:

4 days

Result:

Had a small but nonsignificant promitotic effect at 3nM,while treatment at higher dosages (10 and 30nM) 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 GABAB receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs,with a biphasic dose-response curve.Oral Lesogaberan (0.08mg/mL;48 hours) protects human islet β-cells from apoptosis in islet grafts in mice.Lesogaberan (7μmol/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:

0.08mg/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:

7μmol/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.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
搜索质检报告(COA)
参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • =
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    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):