TRC 051384
目录号 : GC10481
TRC 051384 是一种热休克蛋白 70 (HSP70) 诱导剂。
Cas No.:867164-40-7
Sample solution is provided at 25 µL, 10mM.
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Target: Hsp70
IC50: N/A
TRC 051384, belonging to substituted 2-propen-1-one class, is a potent inducer of heat shock protein 70 (HSP70) [1]. Induction of HSP70 is a natural response of stressed cells that protects neuronal cells from a variety of insults including acute ischemia. Therefore, induction of HSP70 provides a potential target for the treatment of stroke [1].
In vitro: Induction of HSP70 by TRC 051384 (6.25, and 12.5 μM) involved heat shock factor-1 (HSF1) activation in HeLa cells and led to increasing chaperone and anti-inflammatory activity [1]. Moreover, TRC 051384 (10-50 μM) dose-dependently induced HSPA1B overexpression in endothelial cells as well as leucocyte origin [2].
In vivo: TRC 051384 (9 mg/kg, intra-peritoneal administration) treatment significantly decreased stroke-associated neuronal injury, disability, and increased survival in a rat model of transient ischemic stroke [1]. In addition, TRC 051384 (9 mg/kg, intra-peritoneal administration) delayed thrombus formation without increasing bleeding risk in WT mice [2].
References:
1. Mohanan A, Deshpande S, Jamadarkhana PG, Kumar P, Gupta RC, Chauthaiwale V, et al. Delayed intervention in experimental stroke with TRC 051384--a small molecule HSP70 inducer. Neuropharmacology. 2011;60(6):991-9.
2. Allende M, Molina E, Guruceaga E, Tamayo I, Gonzalez-Porras JR, Gonzalez-Lopez TJ, et al. Hsp70 protects from stroke in atrial fibrillation patients by preventing thrombosis without increased bleeding risk. Cardiovasc Res. 2016;110(3):309-18.
Cell experiment: | HeLa cell transiently co-transfected with heat shock elements-luciferase reporter and normalization vector, β-galactosidase are treated with vehicle or TRC051384 (12.5 and 25 μM) for 4 hours. Cell lysates are then prepared and analyzed for luciferase and β-galactosidase activity[1]. |
Animal experiment: | Rats: Injured hemispheres from vehicle treated animals and TRC051384 treated animals are collected at 10-hour post-initiation of tMCAo. Total RNA from each brain sample is extracted followed by cDNA preparation. Each sample of cDNA is analyzed[1]. |
References: [1]. Mohanan A, et al. Delayed intervention in experimental stroke with TRC051384--a small molecule HSP70 inducer. Neuropharmacology. 2011 May;60(6):991-9. | |
| Cas No. | 867164-40-7 | SDF | |
| 化学名 | (Z)-N'-(2-morpholinoethyl)-N-(4-((E)-3-(6-morpholinopyridin-2-yl)acryloyl)phenyl)carbamimidic acid | ||
| Canonical SMILES | O=C(C1=CC=C(N/C(O)=N/CCN2CCOCC2)C=C1)/C([H])=C([H])/C3=NC(N4CCOCC4)=CC=C3 | ||
| 分子式 | C25H31N5O4 | 分子量 | 465.54 |
| 溶解度 | DMSO : ≥ 100 mg/mL (214.80 mM) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.148 mL | 10.7402 mL | 21.4804 mL |
| 5 mM | 0.4296 mL | 2.148 mL | 4.2961 mL |
| 10 mM | 0.2148 mL | 1.074 mL | 2.148 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet