Laduviglusib - CAS:252917-06-9

规格	价格	是否有货	数量
2mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock

规格

价格

是否有货

数量

2mg

In-stock

5mg

In-stock

10mg

In-stock

25mg

In-stock

50mg

In-stock

Other Forms of Rapamycin:

生物活性

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

体外研究

Laduviglusib (CHIR-99021) inhibits human GSK-3β with K_i values of 9.8 nM. 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. 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 μM.

体内研究

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. 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.

分子式

C₂₂H₁₈Cl₂N₈

分子量

465.34

CAS号

252917-06-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 16.67 mg/mL (35.82 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1490 mL	10.7448 mL	21.4897 mL
5 mM	0.4298 mL	2.1490 mL	4.2979 mL
10 mM	0.2149 mL	1.0745 mL	2.1490 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。-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： 0.5% CMC-Na/saline water
Solubility: 5 mg/mL (10.74 mM); Suspension solution; Need ultrasonic
2.

请依序添加每种溶剂： 20% SBE-β-CD adjusted to pH 4-4.5 with 1 N acetic
Solubility: 5 mg/mL (10.74 mM); Clear solution; Need ultrasonic
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.17 mg/mL (4.66 mM); Clear solution

此方案可获得 ≥ 2.17 mg/mL (4.66 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 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
4.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.47 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
5.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.47 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。

科研文献

纯度： 98%

产品说明书

产品使用指南

Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 74 篇科研文献

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