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PF-05231023
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。
PF-05231023图片
CAS NO:1037589-69-7
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
PF-05231023 是一种基于 PEG 的 PROTAC 接头，可用于 PROTAC 的合成。
Cas No.1037589-69-7
Canonical SMILESO=C(CCN1C(C=CC1=O)=O)NCCOCCOCCC(NC2=CC=C(C=C2)CCC(N3C(CC3)=O)=O)=O
分子式C26H32N4O8
分子量528.55
溶解度DMSO : 125 mg/mL (236.50 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
文献引用
产品描述

PF-05231023, a long-acting fibroblast growth factor 21 (FGF21) analog, is a FGF21-receptor agonist, suitable for development as a potential treatment for T2DM[1][5].

PF-05231023 is a long-acting fibroblast growth factor 21 (FGF21) analog[2].

Administration of native FGF21 and PF-05231023 ( 3 mg/kg or 10 mg/kg ) improves glucose tolerance and liver insulin sensitivity in Zucker rats[3].PF-05231023 (10 mg/kg) shows protective effects on Akita retinas. PF-05231023 (10 mg/kg) decreases retinal inflammation in diabetic mice. PF-05231023 (10 mg/kg) administration reduces retinal IL-1β mRNA expression in Akita mice. PF-05231023 (10 mg/kg) administration increases cone-specific arrestin4 expression in Akita mice. PF-05231023 (10 mg/kg) administration restores photoreceptor morphology in Akita mice. PF-05231023 (10 mg/kg) inhibits oxidative-stress-induced inflammation in photoreceptors. PF-05231023 (10 mg/kg) administration decreases the variability of retinal NRF2 levels and shows a trend (non-significant) towards increased NRF2 levels in Akita mice[4].

[1]. Dong JQ, et al. Pharmacokinetics and pharmacodynamics of PF-05231023, a novel long-acting FGF21 mimetic, in a first-in-human study. Br J Clin Pharmacol. 2015 Nov;80(5):1051-63. [2]. Giragossian C, et al. Mechanistic investigation of the preclinical pharmacokinetics and interspecies scaling of PF-05231023, a fibroblast growth factor 21-antibody protein conjugate. Drug Metab Dispos. 2015 Jun;43(6):803-11. [3]. Bernardo B, et al. FGF21 does not require interscapular brown adipose tissue and improves liver metabolic profile in animal models of obesity and insulin-resistance. Sci Rep. 2015 Jul 8;5:11382. [4]. Fu Z, et al. Fibroblast Growth Factor 21 Protects Photoreceptor Function in Type 1 Diabetic Mice. Diabetes. 2018 May;67(5):974-985. [5]. Sonoda J, et al. FGF21-receptor agonists: an emerging therapeutic class for obesity-related diseases. Horm Mol Biol Clin Investig. 2017 May 19;30(2).