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SB756050
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。
SB756050图片
CAS NO:447410-57-3
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
SB756050是选择性的TGR5激动剂,目前正处于临床一期实验用于治疗二型糖尿病。
Cas No.447410-57-3
Canonical SMILESO=S(N1CCN(S(=O)(C2=CC=C(OC)C(OC)=C2)=O)CCC1)(C3=CC=C(OC)C(OC)=C3)=O
分子式C21H28N2O8S2
分子量500.59
溶解度DMSO : ≥ 150 mg/mL (299.65 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

SB756050 is a selective TGR5 agonist currently in phase 1clinical trials for the treatment of type 2 diabetes.

TGR5 is a bile acid receptor and a potential target for the treatment of type 2 diabetes (T2D)[1].

SB756050 is well‐ olerated; it is readily absorbed, exhibited nonlinear pharmacokinetics with a less than dose‐proportional increase in plasma exposure above 100 mg, and demonstrates no significant changes in exposure when co‐administered with sitagliptin. SB756050 demonstrates highly variable pharmacodynamic effects both within dose groups and between doses, with increases in glucose seen at the two lowest doses and no reduction in glucose seen at the two highest doses. The glucose effects of SB756050 ? sitagliptin are comparable to those of sitagliptin alone, even though gut hormone plasma profiles are different[1].

[1]. Hodge RJ, et al. Safety, Pharmacokinetics, and Pharmacodynamic Effects of a Selective TGR5 Agonist, SB-756050, in Type 2 Diabetes. Clin Pharmacol Drug Dev. 2013 Jul;2(3):213-22.