Laduviglusib monohydrochloride CHIR-99021 monohydrochloride; CT99021 monohydrochloride|cas:1797989-42-4|西域试剂

Laduviglusib monohydrochloride CHIR-99021 monohydrochloride; CT99021 monohydrochloride,99.93%

产品编号：Bellancom-10182A| CAS NO：1797989-42-4| 分子式：C₂₂H₁₉Cl₃N₈| 分子量：501.80

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-10182A	￥600.00	杭州北京（现货）
Bellancom-10182A	￥800.00	杭州北京（现货）
Bellancom-10182A	￥1100.00	杭州北京（现货）
Bellancom-10182A	￥2800.00	杭州北京（现货）
Bellancom-10182A	￥5500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Laduviglusib monohydrochloride CHIR-99021 monohydrochloride; CT99021 monohydrochloride

产品介绍

Laduviglusib (CHIR-99021)monohydrochloride 是一种有效的选择性 GSK-3α/β 抑制剂，IC₅₀ 为 10 nM 和 6.7 nM。Laduviglusib monohydrochloride 对 GSK-3 的选择性比 CDC2，ERK2 和其他蛋白激酶高 500 倍以上。Laduviglusib monohydrochloride 还是一种有效的 Wnt/β-catenin 信号通路激活剂。Laduviglusib monohydrochloride 可增强小鼠和人类胚胎干细胞的自我更新。Laduviglusib monohydrochloride 能诱导细胞自噬 (autophagy)。

生物活性

Laduviglusib (CHIR-99021) monohydrochloride is a potent and selective GSK-3α/β inhibitor with IC₅₀s of 10 nM and 6.7 nM. Laduviglusib monohydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib monohydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib monohydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib monohydrochloride induces autophagy.

体外研究

Laduviglusib monohydrochloride inhibits human GSK-3β with K_i values of 9.8 nM. Laduviglusib monohydrochloride is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites. In vitro kinase assays reveal that Laduviglusib monohydrochloride specifically inhibits GSK3β (IC₅₀=~5 nM) and GSK3α (IC₅₀=~10 nM), with little effect on other kinases^[4]. In the presence of Laduviglusib monohydrochloride 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 monohydrochloride with an IC₅₀ of 4.9 μM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

In ZDF rats, a single oral dose of Laduviglusib (16 mg/kg or 48 mg/kg) monohydrochloride rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration. Laduviglusib (2 mg/kg) monohydrochloride given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). Laduviglusib monohydrochloride treatment significantly blocks crypt apoptosis and accumulation of p-H2AX⁺ cells, and improves crypt regeneration and villus height. Laduviglusib monohydrochloride treatment increases Lgr5⁺ cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h^[5].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 60 mg/mL (119.57 mM; Need ultrasonic)

H₂O : 7.14 mg/mL (14.23 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9928 mL	9.9641 mL	19.9283 mL
5 mM	0.3986 mL	1.9928 mL	3.9857 mL
10 mM	0.1993 mL	0.9964 mL	1.9928 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： PBS
Solubility: 5 mg/mL (9.96 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 3 mg/mL (5.98 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (5.98 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 3 mg/mL (5.98 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (5.98 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 3 mg/mL (5.98 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (5.98 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。