T-448|cas:1597426-53-3|西域试剂

T-448,98.62%

产品编号：Bellancom-122635A| CAS NO：1597426-53-3| 分子式：C₁₇H₂₀N₄OS.1/2C₄H₄O₄| 分子量：386.50

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货号	价格	库存与货期
Bellancom-122635A	￥5500.00	杭州北京（现货）
Bellancom-122635A	￥9800.00	杭州北京（现货）
Bellancom-122635A	￥15000.00	杭州北京（现货）

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T-448

产品介绍

T-448 是赖氨酸特异性去甲基化酶1 (LSD1，一种H3K4去甲基化酶) 不可逆的、口服有效的抑制剂，IC₅₀ 值为 22 nM。T-448能够加强原代培养的大鼠神经元中H3K4的甲基化。

生物活性

T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC₅₀ of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons.

体外研究

T-448 enhances the levels of H3K4 methylation, increased mRNA expression of neural plasticity-related genes including brain derived neurotrophic factor (Bdnf), and ameliorated learning dysfunction.

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

RT-PCR.

Cell Line:	Primary cultured rat neurons.
Concentration:	0-10 μM.
Incubation Time:	1 day treatment.
Result:	Increased Ucp2 H3K4me2 and Ucp2 mRNA significantly.

体内研究
(In Vivo)

T-448 has minimal impact on the LSD1-GFI1B complex and a superior hematological safety profile in mice via the generation of a compact formyl-FAD adduct. T-448 increases brain H3K4 methylation and partially restored learning function in mice with NMDA receptor hypofunction.
T-448 increases H3K4 methylation in the brain without causing hematological side effects even at 100 mg/kg.

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

Animal Model:	NR1-hypo mice.
Dosage:	1, 10 mg/kg.
Administration:	Orally, 3 weeks.
Result:	Dose-dependently increased the H3K4me2 levels around Bdnf, Arc, and Fos genes in the mouse hippocampus. Resulted in partial but statistically significant and dosedependent rescue effects on the rate of correct choices in NR1-hypo mice.

体内研究

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

Animal Model:	NR1-hypo mice.
Dosage:	1, 10 mg/kg.
Administration:	Orally, 3 weeks.
Result:	Dose-dependently increased the H3K4me2 levels around Bdnf, Arc, and Fos genes in the mouse hippocampus. Resulted in partial but statistically significant and dosedependent rescue effects on the rate of correct choices in NR1-hypo mice.

体内研究

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

Animal Model:	NR1-hypo mice.
Dosage:	1, 10 mg/kg.
Administration:	Orally, 3 weeks.
Result:	Dose-dependently increased the H3K4me2 levels around Bdnf, Arc, and Fos genes in the mouse hippocampus. Resulted in partial but statistically significant and dosedependent rescue effects on the rate of correct choices in NR1-hypo mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 16.67 mg/mL (43.13 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5873 mL	12.9366 mL	25.8732 mL
5 mM	0.5175 mL	2.5873 mL	5.1746 mL
10 mM	0.2587 mL	1.2937 mL	2.5873 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 (stored under nitrogen)。-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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.67 mg/mL (4.32 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (4.32 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 16.7 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
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.67 mg/mL (4.32 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (4.32 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 16.7 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.67 mg/mL (4.32 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (4.32 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 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。