|1-(2-吗啉乙基)-3-(4-(3-(6-吗啉吡啶-2-基)丙烯酰基)苯基)脲盐酸盐|CsnPharm

CAS No.: 1333327-56-2

1-(2-Morpholinoethyl)-3-(4-(3-(6-morpholinopyridin-2-yl)acryloyl)phenyl)urea hydrochloride Catalog No. CSN20344

Synonyms: TRC051384 Hydrochloride

TRC051384 is an inducer of heat shock protein Hsp70. it reduces stroke-associated neuronal injury and increases survival in a rat model of transient ischemic stroke and activates heat shock factor-1 and results in elevated chaperone and anti-inflammatory activity.

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生物活性

实验方案

技术信息

生物活性

描述TRC051384 is a potent inducer of HSP70 which can induce HSP70B mRNA expression. Dose-dependent increase of HSP70B can be observed on mRNA level in both HeLa and mixed neuronal cells exposure to 6.25μM and 12.5μM TRC051384 for 4h. Consistent with this, TRC051384 at 25μM can increase the transcriptional activity of HSF-1, the protein HSP70 as the chaperone responsible for, in luciferase assay reporter systems in HeLa cells, as well as lead to a significant recovery from a heat shock. Administration of TRC051384 intraperitoneally significantly reduced stroke associated neuronal injury and disability in a rat model of transient ischemic stroke. Meanwhile the enhanced expression of HSP70 can be observed in the affected region of rats dosed with TRC051384^[1]. Administration with 9mg/kg TRC051384 could delayed thrombus formation in mice^[2].
动物研究
剂量
Mice^[2] (i.p.): 9 mg/kg

给药途径
i.p.

动物药代数据
Animal Rats^[1]
Dose 9 mg/kg
Administration i.p,
T_1/2 2 h
T_max 15 min
参考文献

[1] Allende M, Molina E, et al. Hsp70 protects from stroke in atrial fibrillation patients by preventing thrombosis without increased bleeding risk. Cardiovasc Res. 2016 Jun 1;110(3):309-18.
[2] Mohanan A, Deshpande S, et al. Delayed intervention in experimental stroke with TRC051384--a small molecule HSP70 inducer. Neuropharmacology. 2011 May;60(6):991-9.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9920 mL
- 9.9600 mL
- 19.9201 mL
- 5 mM
- 0.3984 mL
- 1.9920 mL
- 3.9840 mL
- 10 mM
- 0.1992 mL
- 0.9960 mL
- 1.9920 mL

技术信息

CAS号	1333327-56-2	储存条件	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C25H32ClN5O4	运输	蓝冰
分子量	502.01	别名	TRC051384 Hydrochloride

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1-(2-Morpholinoethyl)-3-(4-(3-(6-morpholinopyridin-2-yl)acryloyl)phenyl)urea hydrochloride Catalog No. CSN20344

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