LDN-57444|cas:668467-91-2|西域试剂

LDN-57444,99.28%

产品编号：Bellancom-18637| CAS NO：668467-91-2| 分子式：C₁₇H₁₁Cl₃N₂O₃| 分子量：397.64

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货号	价格	库存与货期
Bellancom-18637	￥950.00	杭州北京（现货）
Bellancom-18637	￥3200.00	杭州北京（现货）
Bellancom-18637	￥5200.00	杭州北京（现货）

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LDN-57444

产品介绍

LDN-57444 是一种可逆的，竞争性的，定向位点的泛素 C 末端水解酶 L1 (UCH-L1) 抑制剂，IC₅₀ 和 K_i 值分别为 0.88 μM 和 0.40 μM；LDN-57444 同时可抑制 UCH-L3 的活性，IC₅₀ 值为 25 μM。

生物活性

LDN-57444 is a reversible, competitive and site-directed inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1), with an IC₅₀ of 0.88 μM and a K_i of 0.40 μM; LDN-57444 also suppresses UCH-L3 activity, with an IC₅₀ of 25 μM.

体外研究

LDN-57444 is a reversible, competitive inhibitor of UCH-L1, with an IC₅₀ of 0.88 μM, and also suppresses UCH-L3 activity, with an IC₅₀ of 25 μM. LDN-57444 (LDN, 5 μM for 1 hr) inhibits 70% of Uch activity in hippocampal slices of the mouse brain. LDN-57444 (5 μM for 2 hr) does not reduce potentiation further in APP/PS1 slices or in wt slices exposed to 200 nM Aβ. LDN-57444 (25-100 μM) inhibits ubiquitin-proteasome activity dose-dependently in SK-N-SH cells. LDN-57444 (50 μM) also induces apoptotic cell death, causes the endoplasmic reticulum stress and results in expression of spliced XBP-1(XBP-1s, 48KD) in SK-N-SH cells.

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

体内研究

LDN-57444 (0.4 mg/kg, i.p.) blocks the beneficial effect of V-Uch-L1, and worsens contextual conditioning performance as the mice are exposed to the context at 1, 7, 14, and 21 days after training.

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

体内研究

LDN-57444 (0.4 mg/kg, i.p.) blocks the beneficial effect of V-Uch-L1, and worsens contextual conditioning performance as the mice are exposed to the context at 1, 7, 14, and 21 days after training.

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 : 25 mg/mL (62.87 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5148 mL	12.5742 mL	25.1484 mL
5 mM	0.5030 mL	2.5148 mL	5.0297 mL
10 mM	0.2515 mL	1.2574 mL	2.5148 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： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.29 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。