CCT020312|cas:324759-76-4|西域试剂

CCT020312,99.28%

产品编号：Bellancom-119240| CAS NO：324759-76-4| 分子式：C₃₁H₃₀Br₂N₄O₂| 分子量：650.40

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货号	价格	库存与货期
Bellancom-119240	￥1800.00	杭州北京（现货）
Bellancom-119240	￥3100.00	杭州北京（现货）
Bellancom-119240	￥9500.00	杭州北京（现货）

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CCT020312

产品介绍

CCT020312 是选择性的 EIF2AK3/PERK 的激活剂。CCT020312 可诱导细胞细胞中 EIF2A 的磷酸化。

生物活性

CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.

体外研究

Treatment of HT29 cells with CCT020312 for 24 hours reveals a concentration-dependent loss of P-S608-pRB signal, with a linear response between 1.8 and 6.1 μM.
CCT020312 treatment effectively inhibits cell proliferation (as measured at 96 hours) even if treatment is for 2 hours only with subsequent compound washout, indicating that CCT020312 is capable of eliciting durable rather than transient cytostasis.
Treatment of HT29 cells with 10 μM CCT020312 for 24 hours reduces the amount of the G1/S cyclins D1, D2, E and A as well as the CDK catalytic subunit CDK2 and increased the level of the CDK inhibitor p27KIP1 present in such cells.

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

体内研究

Treatment of 15-week-old wildtype mice with the PERK activator CCT020312 (1-5 mg/kg; i.p.; once daily for 3 days) leads to increased levels of phosphorylated PERK and NRF2 in brain homogenates.
P301S transgenic mice treated with CCT020312 (2 mg/kg; i.p.; once daily for 6 weeks) performes significantly better in Morris water maze.

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

Animal Model:	9-week-old P301S tau transgenic mice
Dosage:	2 mg/kg
Administration:	Intraperitoneal injection; once daily for 6 weeks
Result:	P301S transgenic mice treated with CCT020312 performed significantly better in Morris water maze.

体内研究

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

Animal Model:	9-week-old P301S tau transgenic mice
Dosage:	2 mg/kg
Administration:	Intraperitoneal injection; once daily for 6 weeks
Result:	P301S transgenic mice treated with CCT020312 performed significantly better in Morris water maze.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (153.75 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5375 mL	7.6876 mL	15.3752 mL
5 mM	0.3075 mL	1.5375 mL	3.0750 mL
10 mM	0.1538 mL	0.7688 mL	1.5375 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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.20 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.20 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。
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: 2.08 mg/mL (3.20 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (3.20 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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。
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: ≥ 2.08 mg/mL (3.20 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.20 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。