類器官CHIR-99021

類器官（Organoids）是指將成體干細胞或多能干細胞在體外三維培養(yǎng)形成的具有一定空間結(jié)構(gòu)的組織類似物。類器官在組織結(jié)構(gòu)、細胞類型、自我更新能力和功能等方面與來源組織高度一致，從而在發(fā)育生物學(xué)、疾病造模、精準醫(yī)學(xué)、藥物研發(fā)、基因和細胞療法、感染和免疫以及再生醫(yī)學(xué)等生物醫(yī)學(xué)的多個領(lǐng)域展現(xiàn)出*的優(yōu)勢。

產(chǎn)品介紹DESCRIPTION

BIOLOGICAL ALTIVITY
In Vitro  
CHIR-99021 inhibits human GSK-3β with K_i values of 9.8 nM^[1]. Laduviglusib is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites.In vitro kinase assays reveal that Laduviglusib specifically inhibits GSK3β (IC₅₀=~5 nM) and GSK3α (IC₅₀=~10 nM), with little effect on other kinases^[4]. In the presence of Laduviglusib the viability of the ES-D3 cells is reduced by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM Laduviglusib with an IC₅₀ of 4.9 mm^[2].
In Vivo
In ZDF rats, a single oral dose of Laduviglusib (16 mg/kg or 48 mg/kg) rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration^[1]. Laduviglusib (2 mg/kg) given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). Laduviglusib treatment significantly blocks crypt apoptosis and accumulation of p-H2AX⁺ cells, and improves crypt regeneration and villus height. Laduviglusib treatment increases Lgr5⁺ cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h^[5].

類器官CHIR-99021