您好，欢迎来到试剂仪器网！ [登录] [免费注册]
试剂仪器网
发布求购
位置：首页 > 产品库 > APD597
立即咨询
咨询类型：
     
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
 
APD597
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
APD597图片
CAS NO:897732-93-3
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
APD597 是一种 GPR119 激动剂，用于治疗 2 型糖尿病，对 hGPR119 的 EC50 为 46 nM。
Cas No.897732-93-3
别名JNJ-38431055
Canonical SMILESO=C(OC(C)C)N(CC1)CCC1OC2=C(OC)C(NC3=CC=C(S(=O)(C)=O)N=C3C)=NC=N2
分子式C21H29N5O6S
分子量479.55
溶解度DMSO : ≥ 19 mg/mL (39.62 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

APD597 is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119.IC50 value: 46 nM (EC50) [1]Target: hGPR119The design and synthesis of a second generation GPR119-agonist clinical candidate for the treatment of diabetes is described. APD597 was selected for preclinical development based on a good balance between agonist potency, intrinsic activity and in particular on its good solubility and reduced drug-drug interaction potential. [1]

References:
[1]. Buzard DJ, et al. Discovery and optimization of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists. Bioorg Med Chem Lett. 2014 Sep 1;24(17):4332-4335.
[2]. Semple G, et al. Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improvedprofile. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1750-1755.
[3]. Huan Y, et al. The dual DPP4 inhibitor and GPR119 agonist HBK001 regulates glycemic control and beta cell function ex and in vivo. Sci Rep. 2017 Jun 28;7(1):4351.