PT 1
目录号 : GC17204
An activator of AMPK
Cas No.:331002-70-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
PT 1 is a selective activator of AMPK with EC50 value of 0.3 μM for AMPK α1β1γ1 [1].
AMP-activated protein kinase (AMPK) is serine/threonine protein kinase that involved in cellular energy homeostasis and acts as an energy sensor. AMPK is a heterotrimer and increases ATP generation [1].
PT 1 is a selective AMPK activator. PT1 activated human AMPK α1394, AMPK α2398 and AMPK(α1β1γ1) with EC50 values of 8, 12 and 0.3 μM, respectively. PT1 exhibited maximum activity against AMPK(α1β1γ1) at concentration up to 5 μM. PT1 exhibited high selectivity for AMPK α catalytic subunit. PT1 activated truncated AMPK α1 subunit proteins including 313-335 aa with EC50 values of 8 μM, which was autoinhibitory domain. In HeLa cells without LKB1, PT1 induced AMPK and ACC phosphorylation, which were independent of LKB1. In human hepatoma HepG2 cells, PT1 dose-dependently reduced triacylglycerol and cholesterol content and induced AMPK and ACC phosphorylation [1]. In incubated mouse muscle, PT-1 increased γ1-containing AMPK activity and increased the AMPK-dependent phosphorylation of ULK1 on Ser555. However, in HEK293 cells expressing human γ1-, γ2- or γ3-AMPK, PT-1 activated them equally [2].
References:
[1]. Pang T, Zhang ZS, Gu M, et al. Small molecule antagonizes autoinhibition and activates AMP-activated protein kinase in cells. J Biol Chem, 2008, 283(23): 16051-16060.
[2]. Jensen TE, Ross FA, Kleinert M, et al. PT-1 selectively activates AMPK-γ1 complexes in mouse skeletal muscle, but activates all three γ subunit complexes in cultured human cells by inhibiting the respiratory chain. Biochem J, 2015, 467(3): 461-472.
| Cas No. | 331002-70-1 | SDF | |
| 化学名 | 2-chloro-5-((Z)-((Z)-5-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-4-hydroxythiazol-2(5H)-ylidene)amino)benzoic acid | ||
| Canonical SMILES | CC1=CC(C2=CC=C(O2)/C([H])=C(S/3)/C(O)=NC3=N\C4=CC(C(O)=O)=C(Cl)C=C4)=C(N(=O)=O)C=C1C | ||
| 分子式 | C23H16ClN3O6S | 分子量 | 497.91 |
| 溶解度 | DMF: 1 mg/ml,DMSO: 1 mg/ml,DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml,Ethanol: slightly | 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 | 2.0084 mL | 10.042 mL | 20.084 mL |
| 5 mM | 0.4017 mL | 2.0084 mL | 4.0168 mL |
| 10 mM | 0.2008 mL | 1.0042 mL | 2.0084 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。