AZD1656
目录号 : GC60064AZD1656是一种有效的,选择性的,具有口服活性的葡萄糖激酶(glucokinase)激活剂,EC50为60nM,可用于2型糖尿病的研究。
Cas No.:919783-22-5
Sample solution is provided at 25 µL, 10mM.
AZD1656 is a potent, selective and orally active glucokinase activator with an EC50 of 60 nM. AZD1656 has the potential for type 2 diabetes research[1][2][3].
AZD1656 (0-9 mg/kg; oral gavage; daily; for 8 weeks; C57BL/6 mice) treatment shows lowered blood glucose and glucose excursion and raised insulin. Liver mRNA levels for various ChREBP target genes including carbohydrate response element binding protein beta isoform (ChREBP-β), G6pc, Pklr, Acly, Acac and Gpd2 are increased by AZD1656[1]. Animal Model: C57BL/6 mice[1]
[1]. Brian E Ford, et al. Chronic glucokinase activator treatment activates liver Carbohydrate response element binding protein and improves hepatocyte ATP homeostasis during substrate challenge. Diabetes Obes Metab. 2020 Jun 10. [2]. Medicinal Chemistry, et al. Design and Development of the Glucokinase Activator AZD1656. Complete Accounts of Integrated Drug Discovery and Development: Recent Examples from the Pharmaceutical Industry Volume 1, 185-220. [3]. Terri Mitchard, et al. The novel use of a heterozygous knockout mouse for embryofetal development assessment of a glucokinase activator. Birth Defects Res B Dev Reprod Toxicol. 2014 Apr;101(2):152-61.
Cas No. | 919783-22-5 | SDF | |
Canonical SMILES | O=C(NC1=NC=C(C)N=C1)C2=CC(O[C@@H](C)COC)=CC(OC3=NC=C(C(N4CCC4)=O)N=C3)=C2 | ||
分子式 | C24H26N6O5 | 分子量 | 478.5 |
溶解度 | 储存条件 | ||
General tips | 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。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.0899 mL | 10.4493 mL | 20.8986 mL |
5 mM | 0.418 mL | 2.0899 mL | 4.1797 mL |
10 mM | 0.209 mL | 1.0449 mL | 2.0899 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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