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NCGC00379308
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。
NCGC00379308图片
CAS NO:662164-09-2
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品介绍
NCGC00379308 是促甲状腺激素受体 (TSHR) 的正变构调节剂,它通过直接激活 TSHR 启动 β-Arr 1 的易位,并在体外增强 TSH 介导的前成骨细胞分化。
Cas No.662164-09-2
别名2-甲氧基-4-(4-甲基哌嗪-1-基)苯胺,(D3-βArr;NCGC-00379308;NCGC 00379308)
化学名N-(1-phenylethyl)-2-(1-piperazinyl)-4-quinazolinamine
分子式C20H23N5
分子量333.439
溶解度Soluble in DMSO
储存条件Store at -20℃
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

A potent, functionally selective TSH receptor (TSHR) positive allosteric modulator with EC50 of 11.6 uM (β-Arr 1 translocation); does not activate β-Arr 1 translocation to the GLP1R, binds and activates the TSHR and has no agonistic effect on cAMP production nor inhibit TSH-induced cAMP production in DiscoverX1 cells and primary cultures of human thyrocytes; potentiates TSH-induced upregulation of ALPL and OPN mRNA levels, and increases TSH-induced secretion of OPN protein; potentiates the effect of TSH to enhance differentiation of a human preosteoblast in an in vitro model

Reference:
[1]. Neumann S, et al. J Pharmacol Exp Ther. 2018 Jan;364(1):38-45..